Elancheran Ramakrishnan - Design and development of oxobenzimidazoles as novel androgen receptor antagonists

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      Publication Details (including relevant citation   information):

    Medicinal Chemistry   Research

      Volume   25, Issue 4, pp   539-552


        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 Schrödinger 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.

      Address (URL): http://link.springer.com/article/10.1007%2Fs00044-016-1504-3