通过芳环反转和连接法微波辅助合成作为抗癌剂的微管蛋白组装抑制剂
Microwave-assisted synthesis of tubulin assembly inhibitors as anticancer agents by aryl ring reversal and conjunctive approach.
作者信息
Masci Domiziana, Puxeddu Michela, Colla Claudia, Coluccia Antonio, Santelli Martina, Sciò Pietro, Mariotto Elena, Viola Giampietro, Hamel Ernest, Lerose Rosa, Mazzoccoli Carmela, Silvestri Romano, La Regina Giuseppe
机构信息
Department of Basic Biotechnological Sciences, Intensivological and Perioperative Clinics, Catholic University of the Sacred Heart Largo Francesco Vito 1 00168 Rome Italy.
Policlinico Universitario A. Gemelli Foundation-IRCCS 00168 Rome Italy.
出版信息
RSC Med Chem. 2025 Jul 2. doi: 10.1039/d5md00406c.
Microwave-assisted synthesis of new pyrrole and indole derivatives as tubulin assembly inhibitors was performed with remarkably improved yields and short reaction times. In designing the new inhibitors, aryl ring reversal and conjunctive approach notions were applied. (4-(4-Methoxyphenyl)-1-(pyridin-2-yl)-1-pyrrol-3-yl)(3,4,5-trimethoxyphenyl) methanone (4) inhibited [H] colchicine binding by 78% and MCF-7 breast cancer cell growth with an IC of 9.6 nM. Compound 4 also inhibited the growth of HCT116, BX-PC3 and Jurkat cancer cells with IC values of 18, 17 and 41 nM, respectively, and altered the morphology of treated spheroids in both the BX-PC3 and HCT116 cell lines.
通过微波辅助合成新型吡咯和吲哚衍生物作为微管蛋白组装抑制剂，产率显著提高，反应时间缩短。在设计新型抑制剂时，应用了芳环反转和连接方法的概念。(4-(4-甲氧基苯基)-1-(吡啶-2-基)-1-吡咯-3-基)(3,4,5-三甲氧基苯基)甲酮(4)抑制[H]秋水仙碱结合达78%，对MCF-7乳腺癌细胞生长的IC50为9.6 nM。化合物4还分别以18、17和41 nM的IC50值抑制HCT116、BX-PC3和Jurkat癌细胞的生长，并改变了BX-PC3和HCT116细胞系中处理过的球体的形态。
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