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Chapter 9,504

Synthesis and antitumor activity of novel dolastatin 10 analogs

Miyazaki, K.; Kobayashi, M.; Natsume, T.; Gondo, M.; Mikami, T.; Sakakibara, K.; Tsukagoshi, S.

Chemical and Pharmaceutical Bulletin 43(10): 1706-1718

1995

ISSN/ISBN: 0009-2363
PMID: 8536345
DOI: 10.1248/cpb.43.1706
Accession: 009503931
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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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