Design, synthesis, and evaluation of carbamate-substituted analogues of (+)-discodermolide

被引:42
|
作者
Smith, AB
Freeze, BS
LaMarche, MJ
Hirose, T
Brouard, I
Rucker, PV
Xian, M
Sundermann, KF
Shaw, SJ
Burlingame, MA
Horwitz, SB
Myles, DC [1 ]
机构
[1] Univ Penn, Dept Chem, Philadelphia, PA 19104 USA
[2] Kosan Biosci Inc, Hayward, CA 94545 USA
[3] Albert Einstein Coll Med, Dept Mol Pharmacol, Bronx, NY 10461 USA
关键词
D O I
10.1021/ol047686a
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The design, syntheses, and biological evaluation of 22 totally synthetic analogues of the potent microtubule-stabilizing agent (divided by)-discodermolide (1) have been achieved. Structure-activity relationships of the C(19) carbamate were defined. exploiting two synthetically simplified scaffolds. as well as the parent (+)-discodermolide framework.
引用
收藏
页码:311 / 314
页数:4
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