Ge Haibo, Vasandani Veena, Huff Jacquelyn K, Audus Kenneth L, Himes Richard H, Seelig Anna, Georg Gunda I
Department of Medicinal Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045-7582, USA.
Bioorg Med Chem Lett. 2006 Jan 15;16(2):433-6. doi: 10.1016/j.bmcl.2005.09.043. Epub 2005 Nov 3.
7-Deoxypaclitaxel, 10-deacetoxypaclitaxel and 10-deacetoxy-7-deoxypaclitaxel were prepared and evaluated for their ability to promote assembly of tubulin into microtubules, their cytotoxicity against NCI/ADR-RES cells and for their interactions with P-glycoprotein in bovine brain microvessel endothelial cells. The three compounds were essentially equivalent to paclitaxel in cytotoxicity against NCI/ADR-RES cells. They also appeared to interact with P-glycoprotein in the endothelial cells with the two 10-deacetoxy compounds having less interaction than paclitaxel and 7-deoxypaclitaxel.
制备了7-脱氧紫杉醇、10-去乙酰氧基紫杉醇和10-去乙酰氧基-7-脱氧紫杉醇,并对它们促进微管蛋白组装成微管的能力、对NCI/ADR-RES细胞的细胞毒性以及它们与牛脑微血管内皮细胞中P-糖蛋白的相互作用进行了评估。这三种化合物对NCI/ADR-RES细胞的细胞毒性与紫杉醇基本相当。它们似乎也与内皮细胞中的P-糖蛋白相互作用,两种10-去乙酰氧基化合物的相互作用比紫杉醇和7-脱氧紫杉醇少。