Antitumor Agents 270. Novel Substituted 6-Phenyl-4H-furo32-cpyran-4-one Derivatives as Potent and Highly Selective Anti-Breast Cancer Agents

摘要

6-Phenyl-4H-furo[3,2-c]pyran-4-one derivatives based on neo-tashinlactone (>1) were synthesized and evaluated as novel anti-breast cancer agents. Compounds >10-13, >23, >25, and >27 showed potent inhibition against the SK-BR-3 breast cancer cell line. Importantly, >25 and >27 showed the highest cancer cell line selectivity, being approximately 100- to 250-fold more potent against SK-BR-3 (ED50 0.28 and 0.44 μM, respectively) compared with other cancer cell lines tested. In addition, >25 displayed low cytotoxicity against normal breast cell lines 184A1 and MCF10A. Compounds >25 and >27 merit further investigation in our continuing program to generate and develop selective anti-breast cancer agents.