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Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.

作者信息

Gobbi Silvia, Cavalli Andrea, Negri Matthias, Schewe Katarzyna E, Belluti Federica, Piazzi Lorna, Hartmann Rolf W, Recanatini Maurizio, Bisi Alessandra

出版信息

J Med Chem. 2007 Jul 26;50(15):3420-2. doi: 10.1021/jm0702938. Epub 2007 Jun 22.

DOI:10.1021/jm0702938
PMID:17585752
Abstract

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.

摘要

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