Tag: 195.6024

Wang, Lei et al. published their research in Journal of Medicinal Chemistry in 2020 | CAS: 16732-75-5

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Category: indole-building-block

Scaffold Hopping of Natural Product Evodiamine: Discovery of a Novel Antitumor Scaffold with Excellent Potency against Colon Cancer was written by Wang, Lei;Fang, Kun;Cheng, Junfei;Li, Yu;Huang, Yahui;Chen, Shuqiang;Dong, Guoqiang;Wu, Shanchao;Sheng, Chunquan. And the article was included in Journal of Medicinal Chemistry in 2020.Category: indole-building-block This article mentions the following:

Inspired by the natural product evodiamine, a novel antitumor indolopyrazinoquinazolinone scaffold was designed by scaffold hopping. Structure-activity relationship studies led to the discovery of compound 15j, which shows low nanomolar inhibitory activity against the HCT116 cell line. Further antitumor mechanism studies indicated that compound 15j acted by the dual inhibition of topoisomerase 1 and tubulin and induced apoptosis with G2 cell-cycle arrest. The quaternary ammonium salt of compound 15j (compound 15js) exhibited excellent in vivo antitumor activity (TGI = 66.6%) in the HCT116 xenograft model with low toxicity. Indolopyrazinoquinazolinone derivatives represent promising multitargeting antitumor leads for the development of novel antitumor agents. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5Category: indole-building-block).

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Category: indole-building-block

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

Saha, Goutam Kumar et al. published their research in Journal of the Bangladesh Chemical Society in 2000 | CAS: 96187-75-6

6-Chloro-5-methylindoline-2,3-dione (cas: 96187-75-6) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.HPLC of Formula: 96187-75-6

Synthesis of thiazolo[2′,3′:3,4][1,2,4]triazino[5,6-b]indole from 4,5-disubstituted isatin was written by Saha, Goutam Kumar;Rashid, M. D. Abdur;Islam, M. D. Rabiul. And the article was included in Journal of the Bangladesh Chemical Society in 2000.HPLC of Formula: 96187-75-6 This article mentions the following:

Condensation of 4,5-disubstituted isatin (I) with thiosemicarbazide yields the corresponding thiosemicarbazone, which on cyclization with 4% KOH solution gives 1,2,4-triazino[5,6-b]indole-3-thione derivative (II). Reaction of II with 1,2-dibromoethane in DMF affords the desired compound (III). In the experiment, the researchers used many compounds, for example, 6-Chloro-5-methylindoline-2,3-dione (cas: 96187-75-6HPLC of Formula: 96187-75-6).

6-Chloro-5-methylindoline-2,3-dione (cas: 96187-75-6) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.HPLC of Formula: 96187-75-6

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

Shang, Yanguo et al. published their research in Bioorganic Chemistry in 2022 | CAS: 16732-75-5

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C9H6ClNO2

Development of indole-2-carbonyl piperazine urea derivatives as selective FAAH inhibitors for efficient treatment of depression and pain was written by Shang, Yanguo;Wang, Minghui;Hao, Qingjing;Meng, Tao;Li, Lili;Shi, Junwei;Yang, Guoqing;Zhang, Zhilan;Yang, Kan;Wang, Jinxin. And the article was included in Bioorganic Chemistry in 2022.Formula: C9H6ClNO2 This article mentions the following:

Fatty acid amide hydrolase (FAAH), a serine hydrolase with significant role in the hydrolysis of endocannabinoids, is a promising therapeutic target for peripheral and central nervous system related disorders, including pain, neuroinflammation and depression. Employing a structure-based approach, a novel series of indole-2-carbonyl piperazine urea derivatives were designed and synthesized as FAAH inhibitors for the treatment of pain-depression comorbidity. Among them, compound 4i emerged as the most potent inhibitor (IC50 = 0.12 渭M) with fine selectivity vs. CES2, ABHD6, MAGL and the cannabinoid receptor, which also displayed superior metabolic stability in human liver microsome and an adequate pharmacokinetic profile in rodents. Treatment of depressed rats with 4i demonstrated favorable antidepressant-like effects not only by increasing the level of BDNF in the hippocampus but also by restraining the apoptosis of hippocampal neurons. Also, 4i effectively suppressed the LPS-induced neuroinflammation in vitro. Moreover, 4i exhibited potent analgesic activity, which indicated its promising therapeutical application for pain and depression. These meaningful results shed light on FAAH inhibitors as promising pain-depression comorbidity therapeutics. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5Formula: C9H6ClNO2).

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C9H6ClNO2

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

Wang, Zhen et al. published their research in Journal of Medicinal Chemistry in 2019 | CAS: 16732-75-5

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. 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.COA of Formula: C9H6ClNO2

Optimization of Peptidomimetics as Selective Inhibitors for the 尾-Catenin/T-Cell Factor Protein-Protein Interaction was written by Wang, Zhen;Zhang, Min;Wang, Jin;Ji, Haitao. And the article was included in Journal of Medicinal Chemistry in 2019.COA of Formula: C9H6ClNO2 This article mentions the following:

The 尾-catenin/T-cell factor (Tcf) protein-protein interaction (PPI) plays a critical role in the 尾-catenin signaling pathway which is hyperactivated in many cancers and fibroses. Based on compound 1, which was designed to target the Tcf4 G13ANDE17 binding site of 尾-catenin, extensive structure-activity relationship studies have been conducted. As a result, compounds 53 and 57 were found to disrupt the 尾-catenin/Tcf PPI with the Ki values of 0.64 and 0.44 渭M, resp., and exhibit good selectivity for 尾-catenin/Tcf over 尾-catenin/E-cadherin and 尾-catenin/adenomatous polyposis coli (APC) PPIs. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assays revealed that 56, the Et ester of 53, was more potent than 53 in inhibiting viability of most of the Wnt/尾-catenin hyperactive cancer cells. Further cell-based studies indicated that 56 disrupted the 尾-catenin/Tcf PPI without affecting the 尾-catenin/E-cadherin and 尾-catenin/APC PPIs, suppressed transactivation of Wnt/尾-catenin signaling in dose-dependent manners, and inhibited migration and invasiveness of Wnt/尾-catenin-dependent cancer cells. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5COA of Formula: C9H6ClNO2).

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. 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.COA of Formula: C9H6ClNO2

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

Shang, Yanguo et al. published their research in Bioorganic Chemistry in 2022 | CAS: 16732-75-5

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C9H6ClNO2

Development of indole-2-carbonyl piperazine urea derivatives as selective FAAH inhibitors for efficient treatment of depression and pain was written by Shang, Yanguo;Wang, Minghui;Hao, Qingjing;Meng, Tao;Li, Lili;Shi, Junwei;Yang, Guoqing;Zhang, Zhilan;Yang, Kan;Wang, Jinxin. And the article was included in Bioorganic Chemistry in 2022.Formula: C9H6ClNO2 This article mentions the following:

Fatty acid amide hydrolase (FAAH), a serine hydrolase with significant role in the hydrolysis of endocannabinoids, is a promising therapeutic target for peripheral and central nervous system related disorders, including pain, neuroinflammation and depression. Employing a structure-based approach, a novel series of indole-2-carbonyl piperazine urea derivatives were designed and synthesized as FAAH inhibitors for the treatment of pain-depression comorbidity. Among them, compound 4i emerged as the most potent inhibitor (IC50 = 0.12 μM) with fine selectivity vs. CES2, ABHD6, MAGL and the cannabinoid receptor, which also displayed superior metabolic stability in human liver microsome and an adequate pharmacokinetic profile in rodents. Treatment of depressed rats with 4i demonstrated favorable antidepressant-like effects not only by increasing the level of BDNF in the hippocampus but also by restraining the apoptosis of hippocampal neurons. Also, 4i effectively suppressed the LPS-induced neuroinflammation in vitro. Moreover, 4i exhibited potent analgesic activity, which indicated its promising therapeutical application for pain and depression. These meaningful results shed light on FAAH inhibitors as promising pain-depression comorbidity therapeutics. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5Formula: C9H6ClNO2).

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C9H6ClNO2

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

Wang, Zhen et al. published their research in Journal of Medicinal Chemistry in 2019 | CAS: 16732-75-5

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. 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.COA of Formula: C9H6ClNO2

Optimization of Peptidomimetics as Selective Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction was written by Wang, Zhen;Zhang, Min;Wang, Jin;Ji, Haitao. And the article was included in Journal of Medicinal Chemistry in 2019.COA of Formula: C9H6ClNO2 This article mentions the following:

The β-catenin/T-cell factor (Tcf) protein-protein interaction (PPI) plays a critical role in the β-catenin signaling pathway which is hyperactivated in many cancers and fibroses. Based on compound 1, which was designed to target the Tcf4 G13ANDE17 binding site of β-catenin, extensive structure-activity relationship studies have been conducted. As a result, compounds 53 and 57 were found to disrupt the β-catenin/Tcf PPI with the Ki values of 0.64 and 0.44 μM, resp., and exhibit good selectivity for β-catenin/Tcf over β-catenin/E-cadherin and β-catenin/adenomatous polyposis coli (APC) PPIs. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assays revealed that 56, the Et ester of 53, was more potent than 53 in inhibiting viability of most of the Wnt/β-catenin hyperactive cancer cells. Further cell-based studies indicated that 56 disrupted the β-catenin/Tcf PPI without affecting the β-catenin/E-cadherin and β-catenin/APC PPIs, suppressed transactivation of Wnt/β-catenin signaling in dose-dependent manners, and inhibited migration and invasiveness of Wnt/β-catenin-dependent cancer cells. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5COA of Formula: C9H6ClNO2).

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. 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.COA of Formula: C9H6ClNO2

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

Wang, Zhen et al. published their research in Journal of Medicinal Chemistry in 2019 | CAS: 16732-75-5

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. 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.COA of Formula: C9H6ClNO2

Optimization of Peptidomimetics as Selective Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction was written by Wang, Zhen;Zhang, Min;Wang, Jin;Ji, Haitao. And the article was included in Journal of Medicinal Chemistry in 2019.COA of Formula: C9H6ClNO2 This article mentions the following:

The β-catenin/T-cell factor (Tcf) protein-protein interaction (PPI) plays a critical role in the β-catenin signaling pathway which is hyperactivated in many cancers and fibroses. Based on compound 1, which was designed to target the Tcf4 G13ANDE17 binding site of β-catenin, extensive structure-activity relationship studies have been conducted. As a result, compounds 53 and 57 were found to disrupt the β-catenin/Tcf PPI with the Ki values of 0.64 and 0.44 μM, resp., and exhibit good selectivity for β-catenin/Tcf over β-catenin/E-cadherin and β-catenin/adenomatous polyposis coli (APC) PPIs. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assays revealed that 56, the Et ester of 53, was more potent than 53 in inhibiting viability of most of the Wnt/β-catenin hyperactive cancer cells. Further cell-based studies indicated that 56 disrupted the β-catenin/Tcf PPI without affecting the β-catenin/E-cadherin and β-catenin/APC PPIs, suppressed transactivation of Wnt/β-catenin signaling in dose-dependent manners, and inhibited migration and invasiveness of Wnt/β-catenin-dependent cancer cells. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5COA of Formula: C9H6ClNO2).

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. 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.COA of Formula: C9H6ClNO2

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

Shang, Yanguo et al. published their research in Bioorganic Chemistry in 2022 | CAS: 16732-75-5

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C9H6ClNO2

Development of indole-2-carbonyl piperazine urea derivatives as selective FAAH inhibitors for efficient treatment of depression and pain was written by Shang, Yanguo;Wang, Minghui;Hao, Qingjing;Meng, Tao;Li, Lili;Shi, Junwei;Yang, Guoqing;Zhang, Zhilan;Yang, Kan;Wang, Jinxin. And the article was included in Bioorganic Chemistry in 2022.Formula: C9H6ClNO2 This article mentions the following:

Fatty acid amide hydrolase (FAAH), a serine hydrolase with significant role in the hydrolysis of endocannabinoids, is a promising therapeutic target for peripheral and central nervous system related disorders, including pain, neuroinflammation and depression. Employing a structure-based approach, a novel series of indole-2-carbonyl piperazine urea derivatives were designed and synthesized as FAAH inhibitors for the treatment of pain-depression comorbidity. Among them, compound 4i emerged as the most potent inhibitor (IC50 = 0.12 μM) with fine selectivity vs. CES2, ABHD6, MAGL and the cannabinoid receptor, which also displayed superior metabolic stability in human liver microsome and an adequate pharmacokinetic profile in rodents. Treatment of depressed rats with 4i demonstrated favorable antidepressant-like effects not only by increasing the level of BDNF in the hippocampus but also by restraining the apoptosis of hippocampal neurons. Also, 4i effectively suppressed the LPS-induced neuroinflammation in vitro. Moreover, 4i exhibited potent analgesic activity, which indicated its promising therapeutical application for pain and depression. These meaningful results shed light on FAAH inhibitors as promising pain-depression comorbidity therapeutics. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5Formula: C9H6ClNO2).

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C9H6ClNO2

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

Wang, Zhen et al. published their research in Journal of Medicinal Chemistry in 2019 | CAS: 16732-75-5

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. 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.COA of Formula: C9H6ClNO2

Optimization of Peptidomimetics as Selective Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction was written by Wang, Zhen;Zhang, Min;Wang, Jin;Ji, Haitao. And the article was included in Journal of Medicinal Chemistry in 2019.COA of Formula: C9H6ClNO2 This article mentions the following:

The β-catenin/T-cell factor (Tcf) protein-protein interaction (PPI) plays a critical role in the β-catenin signaling pathway which is hyperactivated in many cancers and fibroses. Based on compound 1, which was designed to target the Tcf4 G13ANDE17 binding site of β-catenin, extensive structure-activity relationship studies have been conducted. As a result, compounds 53 and 57 were found to disrupt the β-catenin/Tcf PPI with the Ki values of 0.64 and 0.44 μM, resp., and exhibit good selectivity for β-catenin/Tcf over β-catenin/E-cadherin and β-catenin/adenomatous polyposis coli (APC) PPIs. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assays revealed that 56, the Et ester of 53, was more potent than 53 in inhibiting viability of most of the Wnt/β-catenin hyperactive cancer cells. Further cell-based studies indicated that 56 disrupted the β-catenin/Tcf PPI without affecting the β-catenin/E-cadherin and β-catenin/APC PPIs, suppressed transactivation of Wnt/β-catenin signaling in dose-dependent manners, and inhibited migration and invasiveness of Wnt/β-catenin-dependent cancer cells. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5COA of Formula: C9H6ClNO2).

6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. 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.COA of Formula: C9H6ClNO2

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