Imidazolylmethylbenzophenones as highly potent aromatase Inhibitors
Imidazolylmethylbenzophenones as highly potent aromatase Inhibitors
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DOI：
10.1021/jm0702938
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发表时间：
2007-07-26
影响因子：
7.3
通讯作者：
Bisi, Alessandra
中科院分区：
文献类型：
--
作者：
Gobbi, Silvia;Cavalli, Andrea;Bisi, Alessandra
通过抑制芳香酶抑制肿瘤和血浆雌激素水平是绝经后乳腺癌患者最有效的治疗方法之一。从一种易于合成的二苯甲酮支架出发，合成了一类对17α-羟基酶/17，20-裂解酶(CYP17)具有较高选择性的新型芳香酶抑制剂。化合物1b和1d被证明是迄今为止描述的最有效的抑制剂之一。
Suppression of tumor and plasma estrogen levels by inhibition of aromatase is one of the most effective treatments for postmenopausal breast cancer patients. Starting from an easy, synthetically accessible, benzophenone scaffold, a new class of potent aromatase inhibitors was synthesized, endowed with high selectivity with respect to 17 alpha-hydroxylase/17,20-lyase (CYP17). Compounds 1b and 1d proved to be among the most potent inhibitors described so far.