Antitumor agents. V. Synthesis and antileukemic activity of E-ring-modified (RS)-camptothecin analogues

A Ejima; H Terasawa; M Sugimori; S Ohsuki; K Matsumoto; Y Kawato; M Yasuoka; H Tagawa

doi:10.1248/cpb.40.683

Antitumor agents. V. Synthesis and antileukemic activity of E-ring-modified (RS)-camptothecin analogues

Chem Pharm Bull (Tokyo). 1992 Mar;40(3):683-8. doi: 10.1248/cpb.40.683.

Authors

A Ejima¹, H Terasawa, M Sugimori, S Ohsuki, K Matsumoto, Y Kawato, M Yasuoka, H Tagawa

Affiliation

¹ Exploratory Research Laboratories I, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.

PMID: 1611680
DOI: 10.1248/cpb.40.683

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.

MeSH terms

Animals
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Camptothecin / analogs & derivatives*
Camptothecin / chemical synthesis
Camptothecin / chemistry
Camptothecin / pharmacology*
Drug Screening Assays, Antitumor
Leukemia P388 / drug therapy*
Magnetic Resonance Spectroscopy
Mice
Tumor Cells, Cultured

Substances

Antineoplastic Agents
7-ethyl-10-methoxy-20-deoxyaminocamptothecin
Camptothecin