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

作者：Vanguru Sowmya; Jilla Lavanya; Sajja Yasodakrishna; Bantu Rajashaker; Nagarapu Lingaiah^*; Nanubolu Jagadeesh Babu; Bhaskar Bala; Jain Nishant; Sivan Sreekanth; Manga Vijjulatha

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(4): 792-796.

DOI：10.1016/j.bmcl.2017.01.031

• Benzosuberone
• Piperazine
• beta-Amino alcohol
• Anti -proliferative
• Cell lines
• Molecular modeling

A new series of 14(9-chloro-2,3-dimethy1-6,7-dihydro-5H-benzo[7jannulen-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, H-1 NMR, C-13 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 GI(50) values ranging from 0.010 to 0.097 mu M. 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 beta-tubulin.

• 出版日期2017-2-15