Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Synthesis and Antitumor Activity of Novel Dolastatin 10 Analogs
Koichi MIYAZAKIMotohiro KOBAYASHITsugitaka NATSUMEMasaaki GONDOTakashi MIKAMIKyoichi SAKAKIBARAShigeru TSUKAGOSHI
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JOURNAL FREE ACCESS

1995 Volume 43 Issue 10 Pages 1706-1718

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Abstract
Dolastatin 10 (1) is a potent antineoplastic pentapeptide. Novel dolastatin 10 analogs each modified at one of the constituent amino acid derivatives, were synthesized and their antitumor activity was evaluated against P388 leukemia in mice. The structural requirements for antitumor activity are discussed. Some of the analogs, 31c, 35c, 38b, and 50c showed excellent activity in vivo. Highly active 50c, which lacks the thiazole group of 1, was selected for further development as an antitumor agent.
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© The Pharmaceutical Society of Japan
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