21402-26-6Relevant articles and documents
Design, synthesis and evaluation of tetrahydrocarbazole derivatives as potential hypoglycemic agents
Chen, Rui,Cheng, Fei,Cui, Xing,Du, Yao,Fan, Ling-Ling,Guo, Bing,Li, Shu-Min,Tang, Lei,Wang, Jian-Ta,Wang, Li-Li,Wu, Hao-Shu,Yang, Sheng-Gang,Zhang, Ji-Quan,Zhang, Na-Na
, (2021/07/28)
Two series of tetrahydrocarbazole derivatives have been designed and synthesized based on ZG02, a promising candidate developed in our previous studies. The newly prepared compounds were screened for glucose consumption activity in HepG2 cell lines. Aza-tetrahydrocarbazole compound 12b showed the most potent hypoglycemic activity with a 45% increase in glucose consumption when compared to the solvent control, which had approximately 1.2-fold higher activity than the positive control compounds (metformin and ZG02). An investigation of the potential mechanism indicated that 12b may exhibit hypoglycemic activity via activation of the AMPK pathway. Metabolic stability assays revealed that 12b showed good stability profiles in both artificial gastrointestinal fluids and blood plasma from SD rats. An oral glucose tolerance test (OGTT) was performed and the results further confirmed that 12b was a potent hypoglycemic agent.
AMINATION AND HYDROXYLATION OF ARYLMETAL COMPOUNDS
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Paragraph 0098; 0136; 0137; 0213, (2018/03/25)
In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions.
Design and development of oxobenzimidazoles as novel androgen receptor antagonists
Elancheran,Saravanan,Choudhury, Bhaswati,Divakar,Kabilan,Ramanathan,Das, Babulal,Devi,Kotoky, Jibon
, p. 539 - 552 (2016/03/08)
Antiandrogens are a novel class of anticancer agents that inhibit cancer cell proliferation and induce apoptosis in various cell lines. To find the lead compound from the oxobenzimidazole derivatives, receptor-ligand docking studies were initially performed using Schr?dinger software. The best fit molecules were synthesized and characterized through IR, 1H-NMR, 13C-NMR and HRMS analyses. The structure of compound (9b) was further confirmed by single-crystal XRD analysis. The cell viability of the compounds was determined by MTT assay to find IC50 values against prostate cancer and breast cancer cell lines (PC-3, LNCaP, MCF-7 and MDA-MB-231). The ADME/T property studies were performed to rationalize the inhibitory properties of these compounds. It can be concluded from the study that 9b is the most active compound from the series against PC-3 and LNCaP cell lines.
