1363401-37-9Relevant academic research and scientific papers
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)
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.
Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists
Guo, Chuangxing,Pairish, Mason,Linton, Angelica,Kephart, Susan,Ornelas, Martha,Nagata, Asako,Burke, Benjamin,Dong, Liming,Engebretsen, Jon,Fanjul, Andrea N.
supporting information; experimental part, p. 2572 - 2578 (2012/05/05)
Oxobenzimidazoles (e.g., 1), a novel series of androgen receptor (AR) antagonists, were discovered through de novo design guided by structure-based drug design. The compounds in this series were reasonably permeable and metabolically stable, but suffered
