康普瑞他汀A-4的新型磺酸盐类似物：强效抗有丝分裂剂。
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
作者信息
Gwaltney S L, Imade H M, Barr K J, Li Q, Gehrke L, Credo R B, Warner R B, Lee J Y, Kovar P, Wang J, Nukkala M A, Zielinski N A, Frost D, Ng S C, Sham H L
机构信息
Cancer Research, Abbott Laboratories, Abbott Park, IL 60064-6101, USA.
出版信息
Bioorg Med Chem Lett. 2001 Apr 9;11(7):871-4. doi: 10.1016/s0960-894x(01)00098-1.
Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Importantly, these compounds also inhibit the proliferation of P-glycoprotein positive (+) cancer cells, which are resistant to many other antitumor agents.
已制备了康普瑞他汀A-4的磺酸盐类似物。这些化合物与秋水仙碱和康普瑞他汀A-4竞争微管蛋白上的秋水仙碱结合位点，并且是微管蛋白聚合和细胞增殖的有效抑制剂。重要的是，这些化合物还抑制P-糖蛋白阳性（+）癌细胞的增殖，这些癌细胞对许多其他抗肿瘤药物具有抗性。
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