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A novel piperazine linked β-amino alcohols bearing a benzosuberone scaffolds as anti-proliferative agents.

Research paper by Sowmya S Vanguru, Lavanya L Jilla, Yasodakrishna Y Sajja, Rajashaker R Bantu, Lingaiah L Nagarapu, Jagadeesh Babu JB Nanubolu, Bala B Bhaskar, Nishant N Jain, Sreekanth S Sivan, Vijjulatha V Manga

Indexed on: 25 Jan '17Published on: 25 Jan '17Published in: Bioorganic & Medicinal Chemistry Letters



Abstract

A new series of 1-((9-chloro-2,3-dimethyl-6,7-dihydro-5H-benzo[7]annulen-8-yl)methoxy)-3-(4-phenylpiperzin-1-yl) propan-2-ols (6a-k) have been designed, synthesized and their structures were established by spectroscopic data (FT-IR, (1)H NMR, (13)C NMR, HRMS) and further confirmed by X-ray analysis. The newly synthesized compounds 6a-k were evaluated for their in vitro anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MDA-MB-231 (breast), A549 (lung) and MIAPACA (pancreatic). Among the compounds tested, the compound 6e displayed most potent activity against four cancer cell lines with GI50 values ranging from 0.010 to 0.097μM. The structure and anti-proliferative activity relationship was further supported by in silico molecular docking study of the active compounds against Colchicine binding site of β-tubulin.

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