Scaffolds for microtubule inhibition through extensive modification of the epothilone template

被引:36
作者
Cachoux, F
Isarno, T
Wartmann, M
Altmann, KH
机构
[1] ETH Honggerberg, Inst Pharmaceut Sci, Dept Chem & Appl Biosci, CH-8093 Zurich, Switzerland
[2] Novartis Inst Biomed Res, Basel, Switzerland
关键词
antitumor agents; drug design; epothilones; microtubule stabilizers; natural products; total synthesis;
D O I
10.1002/anie.200501760
中图分类号
O6 [化学];
学科分类号
0703 [化学];
摘要
(Chemical Equation Presented) The microtubule-stabilizing agent 1 was obtained through extensive modification (colored circles) of the structure of natural epothilone. Despite these structural differences, the biological potency of 1 is comparable with that of epothilone A and taxol! © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:7469 / 7473
页数:5
相关论文
共 36 条
[1]
Recent developments in the chemical biology of epothilones [J].
Altmann, KH .
CURRENT PHARMACEUTICAL DESIGN, 2005, 11 (13) :1595-1613
[2]
Epothilones and related structures - a new class of microtubule inhibitors with potent in vivo antitumor activity [J].
Altmann, KH ;
Wartmann, M ;
O'Reilly, T .
BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER, 2000, 1470 (03) :M79-M91
[3]
The merger of natural product synthesis and medicinal chemistry: on the chemistry and chemical biology of epothilones [J].
Altmann, KH .
ORGANIC & BIOMOLECULAR CHEMISTRY, 2004, 2 (15) :2137-2152
[4]
Altmann KH, 2002, HELV CHIM ACTA, V85, P4086, DOI 10.1002/1522-2675(200211)85:11<4086::AID-HLCA4086>3.0.CO
[5]
2-7
[6]
Microtubule-stabilizing agents: a growing class of important anticancer drugs [J].
Altmann, KH .
CURRENT OPINION IN CHEMICAL BIOLOGY, 2001, 5 (04) :424-431
[7]
Synthesis and biological evaluation of highly potent analogues of epothilones B and D [J].
Altmann, KH ;
Bold, G ;
Caravatti, G ;
Flörsheimer, A ;
Guagnano, V ;
Wartmann, M .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (24) :2765-2768
[8]
[Anonymous], [No title captured], Patent No. [DE 4138042, 4138042]
[9]
Breinbauer R, 2002, ANGEW CHEM INT EDIT, V41, P2879
[10]
BREINBAUER R, 2002, ANGEW CHEM, V114, P3002