Day: October 18, 2021

I found the field of Chemistry very interesting. Saw the article Ultrasound promoted and Kit-6 mesoporous silica-supported Fe3O4 magnetic nanoparticles catalyzed cyclocondensation reaction of 4-hydroxycoumarin, 3,4-methylenedioxyphenol, and aromatic aldehydes published in 2021. Category: indole-building-block, Reprint Addresses Abdolmohammadi, S (corresponding author), Islamic Azad Univ, East Tehran Branch, Dept Chem, POB 18735-138, Tehran, Iran.. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde

A new effective approach to synthesize a series of 7-aryl-6H,7H-[1]benzopyrano[4,3-b][1,3]dioxolo[4,5-g][1]benzopyran-6-ones was reported using Fe3O4@SiO2@Kit-6 as heterogeneous catalyst at room temperature under ultrasonic irradiation in aqueous media. This procedure is of great value due to its short reaction time, high yields, simple processing, and the use of easily available and magnetically recyclable heterogeneous catalyst.

About 4-Methoxybenzaldehyde, If you have any questions, you can contact Abdolmohammadi, S; Shariati, S; Mirza, B or concate me.. Category: indole-building-block

Reference:
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

An article Design, synthesis and biological assessment of new selective COX-2 inhibitors including methyl sulfonyl moiety WOS:000600418500058 published article about ORAL DRUGLIKENESS; PREDICTION; DERIVATIVES; SOLUBILITY; DISCOVERY in [Saglik, Begum Nurpelin; Osmaniye, Derya; Levent, Serkan; Cevik, Ulviye Acar; Ozkay, Yusuf; Kaplancikli, Zafer Asim] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey; [Saglik, Begum Nurpelin; Osmaniye, Derya; Levent, Serkan; Cevik, Ulviye Acar; Ozkay, Yusuf] Anadolu Univ, Fac Pharm, Doping & Narcot Cpds Anal Lab, TR-26470 Eskisehir, Turkey; [Cavusoglu, Betul Kaya] Zonguldak Bulent Ecevit Univ, Fac Pharm, Dept Pharmaceut Chem, TR-67600 Zonguldak, Turkey in 2021, Cited 44. Safety of 3,4-Dimethoxybenzaldehyde. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Nonsteroidal anti-inflammatory drugs (NSAIDs) cause peptic lesions in the gastrointestinal mucosa by inhibiting the cyclooxygenase-1 (COX-1) enzyme. Selective COX-2 inhibition causes decreased side effects over current NSAIDs. Therefore, the studies about selective inhibition of COX-2 enzyme are very important for new drug development. The design, synthesis and biological activity evaluation of novel derivatives bearing thiazolylhydrazine-methyl sulfonyl moiety as selective COX-2 inhibitors were aimed in this paper. The structures of synthesized compounds were assigned using different spectroscopic techniques such as H-1 NMR, C-13 NMR and HRMS. In addition, the estimation of ADME parameters for all compounds was carried out using in silico process. The evaluation of in vitro COX-1/COX-2 enzyme inhibition was applied according to the fluorometric method. According to the enzyme inhibition results, synthesized compounds showed the selectivity against COX-2 enzyme inhibition as expected. Compounds 3a, 3e, 3f, 3g, 3i and 3j demonstrated significant COX-2 inhibition potencies. Among them, compound 3a was found to be the most effective derivative with an IC50 value of 0.140 +/- 0.006 mM. Moreover, it was seen that compound 3a displayed a more potent inhibition profile at least 12-fold than nimesulide (IC50 = 1.684 +/- 0.079 mu M), while it showed inhibitory activity at a similar rate of celecoxib (IC50 = 0.132 +/- 0.005 mu M). Molecular modelling studies aided in the understanding of the interaction modes between this compound and COX-2 enzyme. It was found that compound 3a had a significant binding property. In addition, the selectivity of obtained derivatives on COX-2 enzyme could be explained and discussed by molecular docking studies. (C) 2020 Elsevier Masson SAS. All rights reserved.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Saglik, BN; Osmaniye, D; Levent, S; Cevik, UA; Cavusoglu, BK; Ozkay, Y; Kaplancikli, ZA or concate me.. Safety of 3,4-Dimethoxybenzaldehyde

Reference:
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

In 2021.0 ORG LETT published article about VISIBLE-LIGHT PHOTOCATALYSIS; COPPER in [Zheng, Limeng; Xue, Han; Zhou, Bingwei; Luo, Shu-Ping; Jin, Hongwei; Liu, Yunkui] Zhejiang Univ Technol, Coll Chem Engn, State Key Lab Breeding Base Green Chem Synth Tech, Hangzhou 310014, Peoples R China in 2021.0, Cited 62.0. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5. HPLC of Formula: C8H8O2

An efficient, mild, and atom-economical synthesis of benzo[b]fluorenols from 1,6-enynes has been developed under photocatalytic conditions. A single P/N heteroleptic Cu(I)-photosensitizer might exhibit both energy-transfer and photoredox catalytic activities in the formation of benzo[b]fluorenols.

HPLC of Formula: C8H8O2. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Zheng, LM; Xue, H; Zhou, BW; Luo, SP; Jin, HW; Liu, YK or concate me.

Reference:
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

Recommanded Product: 3,4-Dimethoxybenzaldehyde. Authors Liu, Y; Zhang, Y; Huang, QW; Gou, CA; Li, QZ; Dai, QS; Leng, HJ; Li, JL in WILEY-V C H VERLAG GMBH published article about in [Liu, Yue; Zhang, Ying; Huang, Qian-Wei; Gou, Chuan; Li, Qing-Zhu; Dai, Qing-Song; Leng, Hai-Jun; Li, Jun-Long] Chengdu Univ, Sichuan Ind Inst Antibiot, Sch Pharm, Antibiot Res & Reevaluat Key Lab Sichuan Prov, Chengdu 610106, Peoples R China in 2021.0, Cited 77.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Asymmetric construction of pharmacologically interesting tetrahydrofuranyl spirooxindole frameworks has been achieved through organocatalytic [3+2] annulations of the readily available 3-hydroxyoxindoles and pyrrolidone-derived cyclic ketolactams. A variety of chiral spiro tetrahydrofuranyl products, which contain four contiguous stereocenters including two tetrasubstituted carbon centers, have been rapidly synthesized with remarkable results (up to 99% yield, >95:5 dr, and 99:1 er). Synthetic derivatization of the hemiketal moiety enables the installation of various halogen atoms into the structurally complex molecules in a stereospecific manner. Preliminary screening of anticancer bioactivity was performed, and 4 w showed obvious inhibitory capacity to the proliferation on a panel of cancer cell lines.

Recommanded Product: 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Liu, Y; Zhang, Y; Huang, QW; Gou, CA; Li, QZ; Dai, QS; Leng, HJ; Li, JL or concate me.

Reference:
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

Authors Gong, YX; Zhu, ZD; Qian, Q; Tong, WQ; Gong, HG in AMER CHEMICAL SOC published article about in [Gong, Yuxin; Zhu, Zhaodong; Qian, Qun; Tong, Weiqi; Gong, Hegui] Shanghai Univ, Ctr Supramol Chem & Catalysis, Dept Chem, Shanghai 200444, Peoples R China in 2021.0, Cited 36.0. Name: Mequinol. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5

We describe here the facile construction of sterically hindered tertiary alkyl ethers and thioethers via the Zn(OTf)(2)-catalyzed coupling of alcohols/phenols with unactivated tertiary alkyl bromides and the Cu(OTf)(2)-catalyzed thiolation of unactivated tertiary alkyl oxalates with thiols. The present protocol represents one of the most effective unactivated tertiary C(sp(3))-heteroatom bond-forming conditions via readily accessible Lewis acid catalysis that is surprisingly less developed.

Name: Mequinol. About Mequinol, If you have any questions, you can contact Gong, YX; Zhu, ZD; Qian, Q; Tong, WQ; Gong, HG or concate me.

Reference:
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

In 2020.0 CATAL TODAY published article about METAL-ORGANIC FRAMEWORK; GOLD NANOPARTICLES; NANOPOROUS CARBON; ROOM-TEMPERATURE; EFFICIENT; CO; NITROGEN; SURFACE; SIZE; NANOCLUSTERS in [Chen, Fengfeng; Lu, Qingwen; Fan, Ting; Fang, Ruiqi; Li, Yingwei] South China Univ Technol, Sch Chem & Chem Engn, State Key Lab Pulp & Paper Engn, Guangzhou 510640, Peoples R China in 2020.0, Cited 50.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6. Application In Synthesis of Benzyl Alcohol

Here we report a novel approach to synthesize Au NPs immobilized on N-doped carbon materials. In this strategy, an ionic liquid (IL) [Bmim][AuCl4] was selected as the precursor for Au NPs and porous framework of ZIF-8 as the host for the IL. Raman spectroscopy, transmission electron microscopy, N-2 physical absorption and Fourier infrared spectra confirmed that the IL was successfully incorporated in the ZIF-8 pores. Followed by a thermal treatment under inert atmosphere, highly dispersed Au NPs were obtained and stabilized by nitrogen species from the carbonization of organic ligand in the metal-organic frameworks (MOFs). The [Bmim][AuCl4]@ ZIF-8-6.25%-T materials exhibited high catalytic activity for the selective aerobic oxidation of alcohols, affording excellent yields (up to > 99%) under atmospheric air and base-free conditions. Catalytic reaction along with catalyst characterization results revealed a strong interaction between Au NPs and N species. TEM, XRD and XPS characterization results further suggested that the N species could not only prevent the Au NPs from aggregation, but also further enhance the reaction activity.

Application In Synthesis of Benzyl Alcohol. About Benzyl Alcohol, If you have any questions, you can contact Chen, FF; Lu, QW; Fan, T; Fang, RQ; Li, YW or concate me.

Reference:
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

I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Synthesis, anticancer activity and molecular docking studies on 1,2-diarylbenzimidazole analogues as anti-tubulin agents published in 2019.0. Formula: C7H6O2, Reprint Addresses Wang, ZC; Zhu, HL (corresponding author), Nanjing Univ, Sch Life Sci, State Key Lab Pharmaceut Biotechnol, Nanjing 210023, Jiangsu, Peoples R China.; Jiang, AQ (corresponding author), Nanjing Univ, Med Sch, Nanjing 210093, Jiangsu, Peoples R China.. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde

Twenty-four 1,2-diarylbenzimidazole derivatives were designed, synthesized and biologically evaluated. It turned out that most of them were potential anticancer drugs. Among them, compound c24 showed the highest anti-tumor activity (GI(50) = 0.71-2.41 mu M against HeLa, HepG2, A549 and MCF-7 cells), and low toxicity to normal cells (CC50 > 100 mu M against L02 cells). In the microtubule binding assay, c24 showed the most potent inhibition of microtubule polymerization (IC50 = 8.47 mu M). The binding ability of compound c24 to tubulin crystal was verified by molecular docking simulation experiment. Further studies on HepG2 and HeLa cells showed that compound c24 could cause mitotic arrest of tumor cells to G2/M phase then inducing apoptosis. To sum up, compound c24 is a promising microtubule assembly inhibitor.

Formula: C7H6O2. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Zhang, YL; Yang, R; Xia, LY; Man, RJ; Chu, YC; Jiang, AQ; Wang, ZC; Zhu, HL or concate me.

Reference:
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

An article Study of synergetic effect and comparison of novel sulfonated and carboxylated bulky diamine-diol and piperazine in preparation of negative charge NF membrane WOS:000468714100031 published article about COMPOSITE NANOFILTRATION MEMBRANES; IMPROVED WATER FLUX; INTERFACIAL POLYMERIZATION; ANTIFOULING PROPERTY; DESALINATION; PERFORMANCE; REJECTION; MELAMINE; REMOVAL; MONOMER in [Rezania, Hamidreza (Jafar); Shockravi, Abbas] Kharazmi Univ, Dept Organ Chem, Fac Chem, POB 15719-14911, Tehran, Iran; [Vatanpour, Vahid] Kharazmi Univ, Dept Appl Chem, Fac Chem, POB 15719-14911, Tehran, Iran; [Ehsani, Mortez] Iran Polymer & Petrochem Inst, POB 14965-115, Tehran, Iran in 2019.0, Cited 58.0. Application In Synthesis of 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4

Two new sulfonated (SDA) and carboxylated (CDA) aromatic diamine-diol monomers were synthesized and applied to prepare thin-film composite (TFC) nanofiltration (NF) membranes with improved antifouling and performance properties. The interfacial polymerization method was used to make sulfonated and carboxylated TFC-NF membranes with reaction of trimesoyl chloride (TMC) in the organic phase with amine and hydroxyl agents in the aqueous phase. Herein, for the first time, a comparison between carboxylated and sulfonated TFC was carried out. Moreover, the probability of synergetic effect between these two synthetic monomers (CDA and SDA) and piperazine monomer was studied (the sulfonated monomer and piperazine showed a synergetic effect). The outcomes of flux recovery ratio (FRR), flux and contact angle showed that in the presence of newly synthesized monomers, membrane hydrophilicity considerably improved. The salt retention sequence for all membranes was Na2SO4 NaCl > CaCl2, which means all membranes had a negative charge. Among the five prepared TFC membranes (SDA, CDA, PIP, SDA/PIP, and CDA/PIP), the SDA/PIP showed the best salt rejection (97% Na2SO4) with flux (50 Lm(-2)h(-1)) and 91% FRR, at operating pressure of 10 bars. Although the SDA showed the highest permeability (62 Lm(-2) h(-1)) and FRR of 92%, it presented the lowest Na2SO4 rejection. The results indicated that mixing carboxylated monomers with PIP caused deterioration in properties, while mixing sulfonated monomer with PIP enhanced the performances of the related TFC. Better permeability of the membrane made by newly synthesized monomers is ascribed to the existence of strong hydrophilic sulfonic acid, carboxylic acid and terminal hydroxyls, and amine groups at polyamide top layer producing enhanced membrane antifouling properties.

Application In Synthesis of 4′-Hydroxyacetophenone. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Rezania, H; Vatanpour, V; Shockravi, A; Ehsani, M or concate me.

Reference:
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

Application In Synthesis of 4-Methoxybenzaldehyde. I found the field of Chemistry very interesting. Saw the article Choline chloride/pentaerythritol: a deep eutectic solvent for the synthesis of pyran and chromene derivatives published in 2021, Reprint Addresses Yavari, I (corresponding author), Tarbiat Modares Univ, Dept Chem, Tehran, Iran.. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde.

A novel deep eutectic solvent system was prepared by mixing choline chloride as a hydrogen-bond acceptor with 2,2-bis(hydroxymethyl)propane-1,3-diol (pentaerythritol) as a hydrogen-bond donor. This green solvent was used for the one-pot synthesis of pyran and chromene derivatives from aromatic aldehydes, 1,3-dicarbonyl compounds, and malononitrile. The solvent was readily recycled and can be reused three times without significant loss of activity or mass. This procedure offers advantages such as environmental friendliness, shorter reaction times, and higher yields.

Application In Synthesis of 4-Methoxybenzaldehyde. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Azimzadeh-Sadeghi, S; Yavari, I or concate me.

Reference:
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

Formula: C9H7NO2. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Design, synthesis and biological evaluation of fused naphthofuro[3,2-c]quinoline-6,7,12-triones and pyrano[3,2-c]quinoline-6,7,8,13-tetraones derivatives as ERK inhibitors with efficacy in BRAF-mutant melanoma published in 2019, Reprint Addresses Aly, AA (corresponding author), Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt.; Kaoud, TS (corresponding author), Univ Texas Austin, Div Chem Biol & Med Chem, Austin, TX 78712 USA.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one.

Approximately 60% of human cancers exhibit enhanced activity of ERK1 and ERK2, reflecting their multiple roles in tumor initiation and progression. Acquired drug resistance, especially mechanisms associated with the reactivation of the MAPK (RAF/MEK/ERK) pathway represent a major challenge to current treatments of melanoma and several other cancers. Recently, targeting ERK has evolved as a potentially attractive strategy to overcome this resistance. Herein, we report the design and synthesis of novel series of fused naphthofuro[3,2-c] quinoline-6,7,12-triones 3a-f and pyrano[3,2-c]quinoline-6,7,8,13-tetraones 5a,b and 6, as potential ERK inhibitors. New inhibitors were synthesized and identified by different spectroscopic techniques and X-ray crystallography. They were evaluated for their ability to inhibit ERK1/2 in an in vitro radioactive kinase assay. 3b and 6 inhibited ERK1 with IC50s of 0.5 and 0.19 mu M, and inhibited ERK2 with IC50s of 0.6 and 0.16 mu M respectively. Kinetic mechanism studies revealed that the inhibitors are ATP-competitive inhibitors where 6 inhibited ERK2 with a K-i of 0.09 mu M. Six of the new inhibitors were tested for their in vitro anticancer activity against the NCI-60 panel of tumor cell lines. Compound 3b and 6 were the most potent against most of the human tumor cell lines tested. Moreover, 3b and 6 inhibited the proliferation of the BRAF mutant A375 melanoma cells with IC50s of 3.7 and 0.13 mu M, respectively. In addition, they suppressed anchorage-dependent colony formation. Treatment of the A375 cell line with 3b and 6 inhibited the phosphorylation of ERK substrates p-90RSK and ELK-1 and induced apoptosis in a dose dependent manner. Finally, a molecular docking study showed the potential binding mode of 3b and 6 within the ATP catalytic binding site of ERK2.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS or concate me.. Formula: C9H7NO2

Reference:
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