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Chemical and Pharmaceutical Bulletin
Vol. 43 (1995) No. 10 P 1706-1718

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http://doi.org/10.1248/cpb.43.1706

Synthesis and Antitumor Activity of Novel Dolastatin 10 Analogs

Koichi MIYAZAKI, Motohiro KOBAYASHI, Tsugitaka NATSUME, Masaaki GONDO, Takashi MIKAMI, Kyoichi SAKAKIBARA, Shigeru TSUKAGOSHI

1) Research Department, Teikoku Hormone Mfg. Co., Ltd., 2) Research Department, Teikoku Hormone Mfg. Co., Ltd., 3) Research Department, Teikoku Hormone Mfg. Co., Ltd., 4) Research Department, Teikoku Hormone Mfg. Co., Ltd., 5) Research Department, Teikoku Hormone Mfg. Co., Ltd., 6) Research Department, Teikoku Hormone Mfg. Co., Ltd., 7) Cancer Chemotherapy Center, Cancer Institute, Japanese Foundation for Cancer Research

Released 2008/03/31  
received 1995/04/11   accepted 1995/05/24

Keywords: dolastatin 10 analog, antitumor agent, P388 leukemia, β-phenethylamide analog


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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