Total synthesis and biological assessment of benzimidazole-based analogues of epothilone A: Ambivalent effects on cancer cell growth inhibition

被引：29

作者：

Cachoux, F

Isarno, T

Wartmann, M

Altmann, KH

机构：

[1] ETH Honggerberg, ETH Zurich, Dept Chem & Appl Biosci, Inst Pharmaceut Sci, CH-8093 Zurich, Switzerland

[2] Novartis Inst Biomed Res, Oncol DA, Basel, Switzerland

来源：

CHEMBIOCHEM | 2006年 / 7卷 / 01期

关键词：

antitumor agents; drug discovery; epothilones; microtubule stabilizer; natural products; total synthesis;

D O I：

10.1002/cbic.200500351

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：

Benzimidazole-based analogues of cis- and trans-Epo A, 2 and 3, have been prepared through stereoselective total synthesis. Both compounds are highly potent antiproliferative agents, but the effects of side-chain replacement on cellular activity are ambivalent. While significantly enhanced potency is observed against a drug-sensitive human cancer cell line, 2 and 3 more susceptible to P-gp-mediated drug efflux than Epo A or frans-Epo A. © 2006 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：54 / 57

页数：4

共 2 条

[1] Total synthesis and biological assessment of cyclopropane-based epothilone analogues - Modulation of drug efflux through polarity adjustments
Cachoux, Frederic
Isarno, Thomas
Wartmann, Markus
Altmann, Karl-Heinz
SYNLETT, 2006, (09) : 1384 - 1388
[2] Synthesis and cancer cell growth inhibition effects of acetogenin analogs bearing ethylene glycol units for enhancing the water solubility
Matsumoto, Takuya
Akatsuka, Akinobu
Dan, Shingo
Iwasaki, Hiroki
Yamashita, Masayuki
Kojima, Naoto
TETRAHEDRON, 2020, 76 (13)

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