Halohydrin and oxime derivatives of radicicol: Synthesis and antitumor activities

被引:95
作者
Agatsuma, T
Ogawa, H
Akasaka, K
Asai, A
Yamashita, Y
Mizukami, T
Akinaga, S
Saitoh, Y
机构
[1] Kyowa Hakko Kogyo Co Ltd, Tokyo Res Labs, Machida, Tokyo 1948533, Japan
[2] Kyowa Hakko Kogyo Co Ltd, Pharmaceut Res Inst, Nagaizumi, Shizuoka 4118731, Japan
关键词
D O I
10.1016/S0968-0896(02)00260-2
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Novel halohydrin and oxime derivatives of radicicol (1) were prepared and evaluated for their v-src tyrosine kinase inhibitory, antiproliferative, and antitumor activities. Some of the resulting derivatives showed significantly improved antitumor activities than those of 1 in vitro as tested in a cell proliferation assay and in vivo using sc-inoculated human breast carcinoma and epidermoid tumor models. Design and synthesis of radicicol-based novel affinity probes are also described. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3445 / 3454
页数:10
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