新型第二代紫杉烷类化合物的合成及其构效关系
Synthesis and structure-activity relationships of new second-generation taxoids.
作者信息
Ojima I, Wang T, Miller M L, Lin S, Borella C P, Geng X, Pera P, Bernacki R J
机构信息
Department of Chemistry, State University of New York at Stony Brook, 11794-3400, USA.
出版信息
Bioorg Med Chem Lett. 1999 Dec 20;9(24):3423-8. doi: 10.1016/s0960-894x(99)00629-0.
A series of second-generation taxoids bearing a substituent on the C-2-benzoyl group and modifications at C-3'/C-10 positions was synthesized. These taxoids exhibited 2-3 orders of magnitude higher potency than that of paclitaxel against drug-resistant human breast cancer cell lines. It is also noteworthy that three taxoids showed almost no difference in activity against drug-resistant and drug-sensitive cell lines, which are categorized as "advanced second generation taxoids".
合成了一系列在C-2-苯甲酰基上带有取代基且在C-3'/C-10位有修饰的第二代紫杉烷类化合物。这些紫杉烷类化合物对耐药性人乳腺癌细胞系的活性比紫杉醇高2-3个数量级。同样值得注意的是，三种紫杉烷类化合物对耐药和敏感细胞系的活性几乎没有差异，这些化合物被归类为“先进的第二代紫杉烷类”。
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