| Literature DB >> 18602831 |
M Vijaya Bhaskar Reddy1, Chung-Ren Su, Wen-Fei Chiou, Yi-Nan Liu, Rosemary Yin-Hwa Chen, Kenneth F Bastow, Kuo-Hsiung Lee, Tian-Shung Wu.
Abstract
The chalcone skeleton (1,3-diphenyl-2-propen-1-one) is a unique template that is associated with various biological activities. We synthesized Mannich bases of heterocyclic chalcones (9-47) using a one-step Claisen-Schmidt condensation of heterocyclic aldehydes with Mannich bases of acetophenones, and tested the target compounds for cytotoxicity against three human cancer cell lines (prostate, PC-3; breast, MCF-7; nasopharynx, KB) and a multi-drug resistant subline (KB-VIN). Out of the 39 chalcones synthesized, 31 compounds showed potent activity against at least one cell line with IC(50) values ranging from 0.03 to 3.80 microg/mL. Structure-activity relationships (SAR) are also discussed.Entities:
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Year: 2008 PMID： 18602831 DOI： 10.1016/j.bmc.2008.06.018
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641