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新型芳香酶抑制剂。芳基取代的吡咯里嗪和中氮茚衍生物的合成及生物活性。

New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives.

作者信息

Sonnet P, Dallemagne P, Guillon J, Enguehard C, Stiebing S, Tanguy J, Bureau R, Rault S, Auvray P, Moslemi S, Sourdaine P, Séralini G E

机构信息

Centre d'Etudes et de Recherche sur le Médicament de Normandie, Laboratoire de Pharmacochimie, UFR des Sciences Pharmaceutiques, Caen, France.

出版信息

Bioorg Med Chem. 2000 May;8(5):945-55. doi: 10.1016/s0968-0896(00)00024-9.

DOI:10.1016/s0968-0896(00)00024-9
PMID:10882007
Abstract

We report herein the design and the synthesis of some aryl-substituted pyrrolizine and indolizine derivatives, on the basis of a hypothetical pharmacophore structure designed to fit the catalytic site of the human cytochrome P450 aromatase. The in vitro biological evaluation of these compounds allowed us to point out two new potent non-steroidal aromatase inhibitors, MR 20494 and MR 20492, with IC50 values in the range of 0.1 microM.

摘要

本文报道了一些芳基取代的吡咯里嗪和中氮茚衍生物的设计与合成，其基于一个旨在契合人细胞色素P450芳香化酶催化位点的假设药效团结构。对这些化合物的体外生物学评价使我们发现了两种新的强效非甾体芳香化酶抑制剂，MR 20494和MR 20492，其IC50值在0.1微摩尔范围内。

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