Synthesis, biological evaluation and mechanism studies of deoxytylophorinine and its derivatives as potential anticancer agents.

ABSTRACT: Previous studies indicated that (+)-13a-(S)-deoxytylophorinine (1) showed profound anti-cancer activities both in vitro and in vivo and could penetrate the blood brain barrier to distribute well in brain tissues. CNS toxicity, one of the main factors to hinder the development of phenanthroindolizidines, was not obviously found in 1. Based on its fascinating activities, thirty-four derivatives were designed, synthesized; their cytotoxic activities in vitro were tested to discover more excellent anticancer agents. Considering the distinctive mechanism of 1 and interesting SAR of deoxytylophorinine and its derivatives, the specific impacts of these compounds on cellular progress as cell signaling transduction pathways and cell cycle were proceeded with seven representative compounds. 1 as wel

SUBMITTER: Lv H 

PROVIDER: S-EPMC3261902 | biostudies-literature | 2012

REPOSITORIES: biostudies-literature