Synthesis and Biological Evaluation of 4β-N-Acetylamino Substituted Podophyllotoxin Derivatives as Novel Anticancer Agents.

ABSTRACT: A series of novel podophyllotoxin derivatives obtained by 4β-N-acetylamino substitution at C-4 position was designed, synthesized, and evaluated for in vitro cytotoxicity against four human cancer cell lines (EC-9706, HeLA, T-24 and H460) and a normal human epidermal cell line (HaCaT). The cytotoxicity test indicated that most of the derivatives displayed potent anticancer activities. In particular, compound 12h showed high activity with IC₅₀ values ranging from 1.2 to 22.8 μM, with much better cytotoxic activity than the control drug etoposide (IC₅₀: 8.4 to 78.2 μM). Compound 12j exhibited a promising cytotoxicity and selectivity profile against T24 and HaCaT cell lines with IC₅₀ values of 2.7 and 49.1 μM, respectively. Compound 12g

SUBMITTER: Wei J 

PROVIDER: S-EPMC6491884 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature