Tag: 191.18

Murar, Claudia E. et al. published their research in Journal of the American Chemical Society in 2014 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Related Products of 4382-54-1

KAHA Ligations That Form Aspartyl Aldehyde Residues as Synthetic Handles for Protein Modification and Purification was written by Murar, Claudia E.;Thuaud, Frederic;Bode, Jeffrey W.. And the article was included in Journal of the American Chemical Society in 2014.Related Products of 4382-54-1 This article mentions the following:

Aldehydes are widely recognized as valuable synthetic handles for the chemoselective manipulation of peptides and proteins. In this report, the authors show that peptides and small proteins containing the aspartic acid semialdehyde (Asa) side chain can be easily prepared by a chemoselective amide-forming ligation that results in the formation of the Asa residue at the ligation site. This strategy employs the 伪-ketoacid-hydroxylamine (KAHA) ligation in combination with a new isoxazolidine monomer that forms a side-chain aldehyde upon ligation. This monomer is easily prepared on a preparative scale by a catalytic, enantioselective approach and is readily introduced onto the N-terminus of a peptide segment by solid-phase peptide synthesis. The ligated product can be further functionalized by bioorthogonal reactions between the aldehyde residue and alkoxyamines or hydrazides. The authors demonstrated that glucagon aldehyde, an unprotected 29-mer peptide prepared by KAHA ligation, can be site specifically and chemoselectively modified with biotin, dyes, aliphatic oximes, and hydroxylamines. The authors further describe a simple and high recovery one-step purification process based on the capture of a 29-mer glucagon aldehyde and a 76-mer ubiquitin aldehyde by an alkoxyamine-functionalized polyethylene glycol resin. The peptide or protein was released from the resin by addition of a hydroxylamine to provide the corresponding oximes. In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Related Products of 4382-54-1).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Related Products of 4382-54-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Morzyk-Ociepa, Barbara et al. published their research in Polyhedron in 2014 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Related Products of 4382-54-1

Crystal structure, infrared and EPR spectra and anticancer activity in vitro of the novel manganese(II) complexes of indolecarboxylic acids was written by Morzyk-Ociepa, Barbara;Kokot, Mariusz;Rozycka-Sokolowska, Ewa;Gielzak-Kocwin, Krystyna;Filip-Psurska, Beata;Wietrzyk, Joanna;Michalska, Danuta. And the article was included in Polyhedron in 2014.Related Products of 4382-54-1 This article mentions the following:

The new complexes of 5-methoxyindole-2-carboxylic acid (5-MeOI2CAH) and indole-2-carboxylic acid (I2CAH) with manganese(II): catena-poly[diaquamanganese(II)-bis(渭2-5-methoxyindole-2-carboxylato-O:O’)], [Mn(5-MeOI2CA)2(H2O)2]n (1) and catena-poly[diaquamanganese(II)-bis(渭2-indole-2-carboxylato-O:O’)], [Mn(I2CA)2(H2O)2]n (2) have been prepared A single crystal x-ray anal. of 1 shows that the complex crystallizes in the monoclinic system, space group P21/c. The 5-MeOI2CA anion acts as a bidentate bridging ligand coordinated to Mn(II) in an abnormal non-planar skew-skew mode, which differs from the coplanar syn-syn, syn-anti and anti-anti bridging modes commonly occurring in metal carboxylates. The FTIR and EPR spectroscopic studies of Mn(II) complexes are reported. In vitro cytotoxicities of 1, 2, 5-MeOI2CAH, I2CAH and their Zn(II) complexes have been evaluated by an MTT assay against the selected human leukemia cell lines: HL-60, MV-4-11, U937, Jurkat, KG-1, U2932 and murine melanoma B16-F0. The two manganese(II) complexes are cytotoxic and their antiproliferative activity against some cell lines (e.g. Jurkat derived from an acute T cell leukemia) is similar to that of cisplatin. In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Related Products of 4382-54-1).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Related Products of 4382-54-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Najafi, Sheyda et al. published their research in Scientific Reports in 2022 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Related Products of 4382-54-1

Discovery of a novel class of benzimidazoles as highly effective agonists of bone morphogenetic protein (BMP) receptor signaling was written by Najafi, Sheyda;Barasa, Leonard;Huang, Sammy Y.;Yoganathan, Sabesan;Perron, Jeanette C.. And the article was included in Scientific Reports in 2022.Related Products of 4382-54-1 This article mentions the following:

Increasing or restoring Bone Morphogenetic Protein receptor signaling is an effective therapy for conditions such as bone fracture and pulmonary arterial hypertension. However, direct use of recombinant BMPs has encountered significant obstacles. Moreover, synthetic, full agonists of BMP receptor signaling have yet to be identified. Here, we report the discovery of a novel class of indolyl-benzimidazoles, synthesized using a one-pot synthetic methodol., which appear to mimic the biochem. and functional activity of BMPs. The first-in-series compounds, SY-LB-35 and SY-LB-57, stimulated significant increases in cell number and cell viability in the C2C12 myoblast cell line. Cell cycle anal. revealed that these compounds induced a shift toward proliferative phases. SY-LB-35 and SY-LB-57 stimulated canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways, similar to BMP2-stimulated responses. Importantly, increases in Smad phosphorylation and cell viability were dependent on type I BMP receptor activity. Thus, these compounds robustly activate intracellular signaling in a BMP receptor-dependent manner and may signify the first known, full agonists of BMP receptor signaling. Moreover, discovery of small mol. activators of BMP pathways, which can be efficiently formulated and targeted to diseased or damaged areas, could potentially substitute recombinant BMPs for treatment of BMP-related pathologies. In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Related Products of 4382-54-1).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Related Products of 4382-54-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Zhao, Yu et al. published their research in European Journal of Medicinal Chemistry in 2021 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Name: 5-Methoxyindole-2-carboxylic acid

Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors was written by Zhao, Yu;Chen, Chin-Ho;Morris-Natschke, Susan L.;Lee, Kuo-Hsiung. And the article was included in European Journal of Medicinal Chemistry in 2021.Name: 5-Methoxyindole-2-carboxylic acid This article mentions the following:

Prior modification of betulinic acid (1), a natural product lead with promising anti-HIV activity, produced 3-O-(3′,3′-dimethylsuccinyl)betulinic acid (bevirimat, 3, III), the first-in-class HIV maturation inhibitor. After 3-resistant variants were found during Phase I and IIa clin. trials, further modification of 3 produced 4 (IV) with improved activity against wild-type and 3-resistant HIV-1. In continued efforts to optimize 1, 63 final products have now been designed, synthesized, and evaluated for anti-HIV-1 replication activity against HIV-1NL4-3 infected MT-4 cell lines. Five known and 21 new derivatives were as or more potent than 3 (EC50 0.065渭M), while eight new derivatives were as or more potent than 4 (EC50 0.019渭M). These derivatives feature expanded structural diversity and chem. space that may improve the antiviral activity and address the growing resistance crisis. Structure-Activity Relationship (SAR) correlations were thoroughly analyzed, and a 3D Quant. SAR model with high predictability was constructed to facilitate further rational design and development of new potent derivatives In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Name: 5-Methoxyindole-2-carboxylic acid).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Name: 5-Methoxyindole-2-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Hamdy, Rania et al. published their research in International Journal of Molecular Sciences in 2020 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid

Design, synthesis and evaluation of new bioactive oxadiazole derivatives as anticancer agents targeting Bcl-2 was written by Hamdy, Rania;Elseginy, Samia A.;Ziedan, Noha I.;El-Sadek, Mohamed;Lashin, Elsaid;Jones, Arwyn T.;Westwell, Andrew D.. And the article was included in International Journal of Molecular Sciences in 2020.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid This article mentions the following:

A series of 2-(1H-indol-3-yl)-5-substituted-1,3,4-oxadiazoles I [R = benzyl, 4-methylphenoxymethyl, 4-nitrophenyl, etc.] were designed, synthesized and tested in-vitro as potential pro-apoptotic Bcl-2 inhibitory anticancer agents based on previously reported compounds Synthesis of the target 1,3,4-oxadiazoles I were readily accomplished through a cyclization reaction of indole carboxylic acid hydrazide with substituted carboxylic acid derivatives RC(O)OH in the presence of phosphorus oxychloride. New compounds I showed a range of IC50 values concentrated in the low micromolar range selectively in Bcl-2 pos. human cancer cell lines. The most potent candidate I [R = 4-trifluorophenyl] showed selective IC50 values of 0.52-0.88渭M against Bcl-2 expressing cell lines with no inhibitory effects in the Bcl-2 neg. cell line. Moreover, I [R = 4-trifluorophenyl] showed binding that was two-fold more potent than the pos. control gossypol in the Bcl-2 ELISA binding affinity assay. Mol. modeling studies helped to further rationalize anti-apoptotic Bcl-2 binding and identified compound I [R = 4-trifluorophenyl] as a candidate with drug-like properties for further investigation as a selective Bcl-2 inhibitory anticancer agent. In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Application In Synthesis of 5-Methoxyindole-2-carboxylic acid).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Najafi, Sheyda et al. published their research in Scientific Reports in 2022 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Related Products of 4382-54-1

Discovery of a novel class of benzimidazoles as highly effective agonists of bone morphogenetic protein (BMP) receptor signaling was written by Najafi, Sheyda;Barasa, Leonard;Huang, Sammy Y.;Yoganathan, Sabesan;Perron, Jeanette C.. And the article was included in Scientific Reports in 2022.Related Products of 4382-54-1 This article mentions the following:

Increasing or restoring Bone Morphogenetic Protein receptor signaling is an effective therapy for conditions such as bone fracture and pulmonary arterial hypertension. However, direct use of recombinant BMPs has encountered significant obstacles. Moreover, synthetic, full agonists of BMP receptor signaling have yet to be identified. Here, we report the discovery of a novel class of indolyl-benzimidazoles, synthesized using a one-pot synthetic methodol., which appear to mimic the biochem. and functional activity of BMPs. The first-in-series compounds, SY-LB-35 and SY-LB-57, stimulated significant increases in cell number and cell viability in the C2C12 myoblast cell line. Cell cycle anal. revealed that these compounds induced a shift toward proliferative phases. SY-LB-35 and SY-LB-57 stimulated canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways, similar to BMP2-stimulated responses. Importantly, increases in Smad phosphorylation and cell viability were dependent on type I BMP receptor activity. Thus, these compounds robustly activate intracellular signaling in a BMP receptor-dependent manner and may signify the first known, full agonists of BMP receptor signaling. Moreover, discovery of small mol. activators of BMP pathways, which can be efficiently formulated and targeted to diseased or damaged areas, could potentially substitute recombinant BMPs for treatment of BMP-related pathologies. In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Related Products of 4382-54-1).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Related Products of 4382-54-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Zhao, Yu et al. published their research in European Journal of Medicinal Chemistry in 2021 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Name: 5-Methoxyindole-2-carboxylic acid

Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors was written by Zhao, Yu;Chen, Chin-Ho;Morris-Natschke, Susan L.;Lee, Kuo-Hsiung. And the article was included in European Journal of Medicinal Chemistry in 2021.Name: 5-Methoxyindole-2-carboxylic acid This article mentions the following:

Prior modification of betulinic acid (1), a natural product lead with promising anti-HIV activity, produced 3-O-(3′,3′-dimethylsuccinyl)betulinic acid (bevirimat, 3, III), the first-in-class HIV maturation inhibitor. After 3-resistant variants were found during Phase I and IIa clin. trials, further modification of 3 produced 4 (IV) with improved activity against wild-type and 3-resistant HIV-1. In continued efforts to optimize 1, 63 final products have now been designed, synthesized, and evaluated for anti-HIV-1 replication activity against HIV-1NL4-3 infected MT-4 cell lines. Five known and 21 new derivatives were as or more potent than 3 (EC50 0.065μM), while eight new derivatives were as or more potent than 4 (EC50 0.019μM). These derivatives feature expanded structural diversity and chem. space that may improve the antiviral activity and address the growing resistance crisis. Structure-Activity Relationship (SAR) correlations were thoroughly analyzed, and a 3D Quant. SAR model with high predictability was constructed to facilitate further rational design and development of new potent derivatives In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Name: 5-Methoxyindole-2-carboxylic acid).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Name: 5-Methoxyindole-2-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Hamdy, Rania et al. published their research in International Journal of Molecular Sciences in 2020 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid

Design, synthesis and evaluation of new bioactive oxadiazole derivatives as anticancer agents targeting Bcl-2 was written by Hamdy, Rania;Elseginy, Samia A.;Ziedan, Noha I.;El-Sadek, Mohamed;Lashin, Elsaid;Jones, Arwyn T.;Westwell, Andrew D.. And the article was included in International Journal of Molecular Sciences in 2020.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid This article mentions the following:

A series of 2-(1H-indol-3-yl)-5-substituted-1,3,4-oxadiazoles I [R = benzyl, 4-methylphenoxymethyl, 4-nitrophenyl, etc.] were designed, synthesized and tested in-vitro as potential pro-apoptotic Bcl-2 inhibitory anticancer agents based on previously reported compounds Synthesis of the target 1,3,4-oxadiazoles I were readily accomplished through a cyclization reaction of indole carboxylic acid hydrazide with substituted carboxylic acid derivatives RC(O)OH in the presence of phosphorus oxychloride. New compounds I showed a range of IC50 values concentrated in the low micromolar range selectively in Bcl-2 pos. human cancer cell lines. The most potent candidate I [R = 4-trifluorophenyl] showed selective IC50 values of 0.52-0.88μM against Bcl-2 expressing cell lines with no inhibitory effects in the Bcl-2 neg. cell line. Moreover, I [R = 4-trifluorophenyl] showed binding that was two-fold more potent than the pos. control gossypol in the Bcl-2 ELISA binding affinity assay. Mol. modeling studies helped to further rationalize anti-apoptotic Bcl-2 binding and identified compound I [R = 4-trifluorophenyl] as a candidate with drug-like properties for further investigation as a selective Bcl-2 inhibitory anticancer agent. In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Application In Synthesis of 5-Methoxyindole-2-carboxylic acid).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Zhao, Yu et al. published their research in European Journal of Medicinal Chemistry in 2021 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Name: 5-Methoxyindole-2-carboxylic acid

Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors was written by Zhao, Yu;Chen, Chin-Ho;Morris-Natschke, Susan L.;Lee, Kuo-Hsiung. And the article was included in European Journal of Medicinal Chemistry in 2021.Name: 5-Methoxyindole-2-carboxylic acid This article mentions the following:

Prior modification of betulinic acid (1), a natural product lead with promising anti-HIV activity, produced 3-O-(3′,3′-dimethylsuccinyl)betulinic acid (bevirimat, 3, III), the first-in-class HIV maturation inhibitor. After 3-resistant variants were found during Phase I and IIa clin. trials, further modification of 3 produced 4 (IV) with improved activity against wild-type and 3-resistant HIV-1. In continued efforts to optimize 1, 63 final products have now been designed, synthesized, and evaluated for anti-HIV-1 replication activity against HIV-1NL4-3 infected MT-4 cell lines. Five known and 21 new derivatives were as or more potent than 3 (EC50 0.065μM), while eight new derivatives were as or more potent than 4 (EC50 0.019μM). These derivatives feature expanded structural diversity and chem. space that may improve the antiviral activity and address the growing resistance crisis. Structure-Activity Relationship (SAR) correlations were thoroughly analyzed, and a 3D Quant. SAR model with high predictability was constructed to facilitate further rational design and development of new potent derivatives In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Name: 5-Methoxyindole-2-carboxylic acid).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Name: 5-Methoxyindole-2-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Hamdy, Rania et al. published their research in International Journal of Molecular Sciences in 2020 | CAS: 4382-54-1

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid

Design, synthesis and evaluation of new bioactive oxadiazole derivatives as anticancer agents targeting Bcl-2 was written by Hamdy, Rania;Elseginy, Samia A.;Ziedan, Noha I.;El-Sadek, Mohamed;Lashin, Elsaid;Jones, Arwyn T.;Westwell, Andrew D.. And the article was included in International Journal of Molecular Sciences in 2020.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid This article mentions the following:

A series of 2-(1H-indol-3-yl)-5-substituted-1,3,4-oxadiazoles I [R = benzyl, 4-methylphenoxymethyl, 4-nitrophenyl, etc.] were designed, synthesized and tested in-vitro as potential pro-apoptotic Bcl-2 inhibitory anticancer agents based on previously reported compounds Synthesis of the target 1,3,4-oxadiazoles I were readily accomplished through a cyclization reaction of indole carboxylic acid hydrazide with substituted carboxylic acid derivatives RC(O)OH in the presence of phosphorus oxychloride. New compounds I showed a range of IC50 values concentrated in the low micromolar range selectively in Bcl-2 pos. human cancer cell lines. The most potent candidate I [R = 4-trifluorophenyl] showed selective IC50 values of 0.52-0.88μM against Bcl-2 expressing cell lines with no inhibitory effects in the Bcl-2 neg. cell line. Moreover, I [R = 4-trifluorophenyl] showed binding that was two-fold more potent than the pos. control gossypol in the Bcl-2 ELISA binding affinity assay. Mol. modeling studies helped to further rationalize anti-apoptotic Bcl-2 binding and identified compound I [R = 4-trifluorophenyl] as a candidate with drug-like properties for further investigation as a selective Bcl-2 inhibitory anticancer agent. In the experiment, the researchers used many compounds, for example, 5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1Application In Synthesis of 5-Methoxyindole-2-carboxylic acid).

5-Methoxyindole-2-carboxylic acid (cas: 4382-54-1) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Application In Synthesis of 5-Methoxyindole-2-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles