Literature DB >> 17585752

Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.

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

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.

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Year:  2007        PMID： 17585752     DOI： 10.1021/jm0702938

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  5 in total

1.  Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.

Authors:  Kevin Bonfield; Erica Amato; Tony Bankemper; Hannah Agard; Jeffrey Steller; James M Keeler; David Roy; Adam McCallum; Stefan Paula; Lili Ma
Journal:  Bioorg Med Chem       Date:  2012-02-27       Impact factor: 3.641

2.  Design, synthesis, and biological evaluation of resveratrol analogues as aromatase and quinone reductase 2 inhibitors for chemoprevention of cancer.

Authors:  Bin Sun; Juma Hoshino; Katie Jermihov; Laura Marler; John M Pezzuto; Andrew D Mesecar; Mark Cushman
Journal:  Bioorg Med Chem       Date:  2010-05-24       Impact factor: 3.641

3.  Aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole and vorozole templates.

Authors:  Paul M Wood; L W Lawrence Woo; Mark P Thomas; Mary F Mahon; Atul Purohit; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-05-23       Impact factor: 3.466

4.  3-Pyridyl substituted aliphatic cycles as CYP11B2 inhibitors: aromaticity abolishment of the core significantly increased selectivity over CYP1A2.

Authors:  Lina Yin; Qingzhong Hu; Rolf W Hartmann
Journal:  PLoS One       Date:  2012-11-01       Impact factor: 3.240

5.  Synthesis and biological evaluation of thieno[3,2-d]- pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones: conformationally restricted 17b-hydroxysteroid dehydrogenase type 2 (17b-HSD2) inhibitors.

Authors:  Enrico Perspicace; Sandrine Marchais-Oberwinkler; Rolf W Hartmann
Journal:  Molecules       Date:  2013-04-16       Impact factor: 4.411
  5 in total

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