Anderson James T, Ting Anthony E, Boozer Sherry, Brunden Kurt R, Danzig Joel, Dent Tom, Harrington John J, Murphy Steven M, Perry Rob, Raber Amy, Rundlett Stephen E, Wang Jianmin, Wang Nancy, Bennani Youssef L
Athersys, Inc., 3201 Carnegie Avenue, Cleveland, Ohio 44115-2634, USA.
J Med Chem. 2005 Apr 21;48(8):2756-8. doi: 10.1021/jm0494220.
Analogues of the natural product noscapine were synthesized, and their potential as antitumor agents were examined. The discovery of a novel regio- and stereoselective O-demethylation led to the synthesis of several O-alkylated analogues that induced an unexpected S-phase arrest of mammalian cells. Compound 4a was the most potent analogue inhibiting cell proliferation at an EC(50) of 1.9 microM.
合成了天然产物那可丁的类似物，并研究了它们作为抗肿瘤剂的潜力。一种新型区域和立体选择性O-去甲基化的发现导致了几种O-烷基化类似物的合成，这些类似物可诱导哺乳动物细胞出现意外的S期阻滞。化合物4a是最有效的类似物，其半数有效浓度（EC50）为1.9 microM，可抑制细胞增殖。
