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Antitumor agents. V. Synthesis and antileukemic activity of E-ring-modified (RS)-camptothecin analogues
A Ejima1, H Terasawa, M Sugimori
1Exploratory Research Laboratories I, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Chemical & Pharmaceutical Bulletin
|March 1, 1992
Abstract:
Several E-ring-modified analogues of (RS)-camptothecin were synthesized by total synthesis via Friedländer condensation and evaluated for cytotoxicity and antitumor activity against P388 mouse leukemia cells. Among them, (RS)-20-deoxyamino-7-ethyl-10-methoxycamptothecin (25c) was found to be more active than (RS)-camptothecin (1) in the in vivo assay.