A structure-activity relationship study of brusatol, an antitumor quassinoid

被引：24

作者：

Hitotsuyanagi, Y ^{[1
]}

Kim, IH ^{[1
]}

Hasuda, T ^{[1
]}

Yamauchi, Y ^{[1
]}

Takeya, K ^{[1
]}

机构：

[1] Tokyo Univ Pharm & Life Sci, Sch Pharm, Tokyo 1920392, Japan

来源：

TETRAHEDRON | 2006年 / 62卷 / 17期

关键词：

bruceantin; brusatol; quassinoid; SAR cytotoxicity;

D O I：

10.1016/j.tet.2006.01.083

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Analogues of brusatol (2) were prepared and examined for their cytotoxic activity by using P-388 murine leukemia cells. The following structure-activity relationships were noted: (i) an enone carbonyl oxygen or an enolic oxygen at C-2 is essential, but an oxygen at C-3 not essential for the activity; (ii) the C-11 beta-hydroxyl group is important for the activity; and (iii) the length of the ester alkoxy side chain at C-21 seems to have a slight effect on the activity. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4262 / 4271

页数：10

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