Asymmetric synthesis and evaluation of alpha-quaternary chiral lactam derivatives as novel anticancer agents

作者:Lee Hwanhyuk; Hwang Su Jung; Jung Jisung; Hong Suckchang; Lee Myungmo; Park Hyeung geun; Lee Hyo Jong; Park Yohan
来源:Archives of Pharmacal Research, 2014, 37(10): 1264-1270.
DOI:10.1007/s12272-013-0274-4

摘要

Asymmetric synthesis of alpha-quaternary chiral lactam derivatives as novel anticancer agents and evaluation of their cytotoxic potentials and spectrums are reported. Among the developed lactam derivatives, the most active new compounds (S)-4m and (S)-4n synthesized via asymmetric phase-transfer catalytic alkylation in very high optical yields (98 % ee) show promising in vitro anticancer activities with low micromolar IC50 values against colon, uterus, lung, and breast human cancer cells.

  • 出版日期2014-10