Plant antitumor agents. 25. Total synthesis and antileukemic activity of ring A substituted camptothecin analogs. Structure-activity correlations

MC Wani, AW Nicholas, G Manikumar…

Index: Wani; Nicholas; Manikumar; Wall Journal of Medicinal Chemistry, 1987 , vol. 30, # 10 p. 1774 - 1779

Full Text: HTML

Citation Number: 145

Abstract

Nineteen racemic ring A substituted analogues of the antitumor agent 2O (S)-camptothecin were prepared by total synthesis and evaluated for in vitro cytotoxic activity against KB cell culture and in vivo antileukemic activity against L1210. These compounds bore a wide variety of substitutents at Cl1 designed to confer upon the ring system a broad range of combinations of electronic, steric, and lipophilic effects. A few Clo-substituted derivatives ...