Literature DB >> 16730987

Estrogen receptor beta-subtype selective tetrahydrofluorenones: use of a fused pyrazole as a phenol bioisostere.

R R Wilkening1, R W Ratcliffe, A K Fried, D Meng, W Sun, L Colwell, S Lambert, M Greenlee, S Nilsson, A Thorsell, M Mojena, C Tudela, K Frisch, W Chan, E T Birzin, S P Rohrer, M L Hammond.   

Abstract

Synthesis of a series of fused pyrazole tetrahydrofluorenone analogs which are potent, ERbeta subtype selective ligands is described. Analogs possessing subnanomolar ERbeta binding, greater than 100-fold ERbeta-selectivity, and oral bioavailability are reported.

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Year:  2006        PMID: 16730987     DOI: 10.1016/j.bmcl.2006.05.036

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Synthesis of Functionalized Alkylidene Indanes and Indanones through Tandem Phosphine-Palladium Catalysis.

Authors:  Yi Chiao Fan; Ohyun Kwon
Journal:  Org Lett       Date:  2015-04-14       Impact factor: 6.005

Review 2.  Development of subtype-selective oestrogen receptor-based therapeutics.

Authors:  Stefan Nilsson; Konrad F Koehler; Jan-Åke Gustafsson
Journal:  Nat Rev Drug Discov       Date:  2011-09-16       Impact factor: 84.694

3.  Optimization of Pyrazoles as Phenol Surrogates to Yield Potent Inhibitors of Macrophage Migration Inhibitory Factor.

Authors:  Vinay Trivedi-Parmar; Michael J Robertson; José A Cisneros; Stefan G Krimmer; William L Jorgensen
Journal:  ChemMedChem       Date:  2018-04-23       Impact factor: 3.466

4.  Structural simplification of bioactive natural products with multicomponent synthesis: dihydropyridopyrazole analogues of podophyllotoxin.

Authors:  Igor V Magedov; Madhuri Manpadi; Elena Rozhkova; Nikolai M Przheval'skii; Snezna Rogelj; Scott T Shors; Wim F A Steelant; Severine Van slambrouck; Alexander Kornienko
Journal:  Bioorg Med Chem Lett       Date:  2006-12-06       Impact factor: 2.823

Review 5.  Versatility or promiscuity: the estrogen receptors, control of ligand selectivity and an update on subtype selective ligands.

Authors:  Hui Wen Ng; Roger Perkins; Weida Tong; Huixiao Hong
Journal:  Int J Environ Res Public Health       Date:  2014-08-26       Impact factor: 3.390

  5 in total

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