4.6 Article

Synthesis, anticancer activity and docking studies of N-phenyl-2-(2-((4-phenyl piperazin-1-yl) methyl)-1H-benzo [d] imidazol-1-yl) acetamides

Journal

JOURNAL OF MOLECULAR STRUCTURE
Volume 1166, Issue -, Pages 362-368

Publisher

ELSEVIER
DOI: 10.1016/j.molstruc.2018.04.057

Keywords

o-phenylene diamine; Phenyl piperazines; Acid-amide coupling; Anticancer activity; Docking

Funding

  1. UGC

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A series of novel N-phenyl-2-(2-((4-phenyl piperazin-1-yl) methyl)-1H-benzo [d] imidazol-1-yl) acet-amides (7a-o) have been synthesized in multiple steps with suitable reaction procedures and well characterized by various analytical techniques. All the synthesized compounds were evaluated for their in vitro anticancer activity against three human cancer cell lines includes human cervical carcinoma (HeLa), human breast carcinoma (MCF-7) and human embryonic kidney (HEK 293) cell lines at various concentrations. The results were shown in terms of percentage cell viability reduction and IC(50)values were compared against standard anti cancer drug doxorubicin. Among all the synthesized compounds, compound 7k has shown highest activity against HeLa and MCF-7. The compounds 7b, 71, 7m, 7n and 7o also showed significant activity over HeLa and MCF-7. Furthermore, the structure and anticancer activity relationship was supported by molecular docking study of the active compounds against quinone reductase-2 (PDB ID 4ZVM) protein. (C) 2018 Published by Elsevier B.V.

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