Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with IC(50) values of 0.7 and 0.6 μM, respectively.
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【Synthesis and biological evaluation of a new series of phenothiazine-containing protein farnesyltransferase inhibitors.].
【一系列新的含吩噻嗪的蛋白质法呢基转移酶抑制剂的合成和生物学评估。】
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DOI：10.1016/j.ejmech.2012.11.008文章类型：杂志文章
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：基于吩噻嗪支架，合成了两个新的人类法呢基转移酶抑制剂家族13a-m和14a-d。化合物14a和14b是人类法呢基转移酶的最有希望的抑制剂，其IC（50）值分别为0.7和0.6μM。
