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化学名
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(1R,5S,6S,7R,10S,14S,16S)-6,10-dihydroxy-5,7,9,9-tetramethyl-14-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-13,17-dioxabicyclo[14.1.0]heptadecane-8,12-dione
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分子式
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C26H39NO6S
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详细内容
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Epothilone A (Epo A) is a naturally occurring microtubule-stabilizing macrolide that was first isolated from the myxobacterium Sorangium cellulosum. The IC50 value of Epothilone A in HCT-116 cell line is 4.4 nM [1].
It has been found that the SKOV-3 human ovarian cancer cells were susceptible to Epothilone A with IC50 value of 20.4 ± 1.4 nM [2]. The antiproliferative capacity of Epothilone A in SKOV-3 cell line (measured as IC50 after 72 h continuous treatment) was six times greater than that of PTX’s. Besides, Epothilone A induced time coursedependent apoptosis and necrosis [2].
References:
[1] Regueiro-Ren A1, Borzilleri RM, Zheng X, Kim SH, Johnson JA, Fairchild CR, Lee FY, Long BH, Vite GD. Synthesis and biological activity of novel epothilone aziridines. Org Lett. 2001 Aug 23;3(17):2693-6.
[2] Rogalska A1, Marczak A, Gajek A, Szwed M, ?liwińska A, Drzewoski J, Jó?wiak Z. Induction of apoptosis in human ovarian cancer cells by new anticancer compounds, epothilone A and B. Toxicol In Vitro. 2013 Feb;27(1):239-49.
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