新型同型喜树碱类似物的合成与生物评价。
Synthesis and biological evaluation of new homocamptothecin analogs.
机构信息
Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, 3663 North Zhongshan Road, East China Normal University, Shanghai 200062, China.
出版信息
Eur J Med Chem. 2012 Aug;54:281-6. doi: 10.1016/j.ejmech.2012.05.002. Epub 2012 May 15.
In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to α position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability.
为了提高同型喜树碱 E 环的稳定性，在环-E 内酯的α位引入吸电子基团-OH 或-OAc。合成了十个新的同型喜树碱类似物。大多数化合物表现出很强的体外抗癌活性和很强的 Topo I 抑制活性，与 CPT、SN-38 和 10-HCPT 相当或优于后者。该系列化合物的稳定性研究也显示出稳定性的显著提高。
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