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Synthesis and biological evaluation of N-(7-indolyl)-3-pyridinesulfonamide derivatives as potent antitumor agents. 2002
Takashi Owa, and
Hiroshi Yoshino, and
Tatsuo Okauchi, and
Tadashi Okabe, and
Yoichi Ozawa, and
Naoko Hata Sugi, and
Kentaro Yoshimatsu, and
Takeshi Nagasu, and
Nozomu Koyanagi, and
Kyosuke Kitoh
Tsukuba Research Laboratories, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba, 300-2635, Ibaraki, Japan. t-owa@hhc.eisai.co.jp
We herein report the synthesis and antitumor activity of E7070 analogues containing a 3-pyridinesulfonamide moiety. E7070 was selected from our sulfonamide-based compound collections, currently undergoing Phase II clinical trials because of its tolerable toxicity profile and some antitumor responses in the Phase I setting. Of the analogues examined, ER-35745, a 6-amino-3-pyridinesulfonamide derivative, demonstrated significant oral efficacy against the HCT116 human colon carcinoma xenograft in nude mice.
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