Literature DB >> 15125923

Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.

Richard Chesworth1, Michael P Zawistoski, Bruce A Lefker, Kimberly O Cameron, Robert F Day, F Michael Mangano, Robert L Rosati, Stacy Colella, Donna N Petersen, Amy Brault, Bihong Lu, Lydia C Pan, Pia Perry, Oicheng Ng, Tessa A Castleberry, Thomas A Owen, Thomas A Brown, David D Thompson, Paul DaSilva-Jardine.   

Abstract

Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER alpha and ER beta selective analogs.

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Year:  2004        PMID: 15125923     DOI: 10.1016/j.bmcl.2004.03.077

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


  10 in total

1.  Tetrahydroisoquinolinone-based steroidomimetic and chimeric microtubule disruptors.

Authors:  Mathew P Leese; Fabrice L Jourdan; Meriel R Major; Wolfgang Dohle; Ernest Hamel; Eric Ferrandis; Ann Fiore; Philip G Kasprzyk; Barry V L Potter
Journal:  ChemMedChem       Date:  2013-10-09       Impact factor: 3.466

2.  Bioactivity-guided mapping and navigation of chemical space.

Authors:  Steffen Renner; Willem A L van Otterlo; Marta Dominguez Seoane; Sabine Möcklinghoff; Bettina Hofmann; Stefan Wetzel; Ansgar Schuffenhauer; Peter Ertl; Tudor I Oprea; Dieter Steinhilber; Luc Brunsveld; Daniel Rauh; Herbert Waldmann
Journal:  Nat Chem Biol       Date:  2009-06-28       Impact factor: 15.040

3.  In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models.

Authors:  Suresh Kumar V K Eyunni; Madhavi Gangapuram; Kinfe K Redda
Journal:  Lett Drug Des Discov       Date:  2014       Impact factor: 1.150

Review 4.  Recent progress in selective estrogen receptor downregulators (SERDs) for the treatment of breast cancer.

Authors:  Irshad Ahmad; Shimy Mathew; Sofia Rahman
Journal:  RSC Med Chem       Date:  2020-03-06

5.  Lasofoxifene: Evidence of its therapeutic value in osteoporosis.

Authors:  Luigi Gennari; Daniela Merlotti; Vincenzo De Paola; Ranuccio Nuti
Journal:  Core Evid       Date:  2010-06-15

Review 6.  Selective estrogen receptor modulator (SERM) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene.

Authors:  Luigi Gennari; Daniela Merlotti; Ranuccio Nuti
Journal:  Clin Interv Aging       Date:  2010-02-02       Impact factor: 4.458

7.  Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.

Authors:  James S Scott; Andrew Bailey; Robert D M Davies; Sébastien L Degorce; Philip A MacFaul; Helen Gingell; Thomas Moss; Richard A Norman; Jennifer H Pink; Alfred A Rabow; Bryan Roberts; Peter D Smith
Journal:  ACS Med Chem Lett       Date:  2015-12-19       Impact factor: 4.345

Review 8.  Selective estrogen receptor modulators for postmenopausal osteoporosis: current state of development.

Authors:  Luigi Gennari; Daniela Merlotti; Fabrizio Valleggi; Giuseppe Martini; Ranuccio Nuti
Journal:  Drugs Aging       Date:  2007       Impact factor: 3.923

9.  Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors.

Authors:  Mathew P Leese; Fabrice Jourdan; Wolfgang Dohle; Meriel R Kimberley; Mark P Thomas; Ruoli Bai; Ernest Hamel; Eric Ferrandis; Barry V L Potter
Journal:  ACS Med Chem Lett       Date:  2011-10-31       Impact factor: 4.345

10.  Silica-supported polyphosphoric acid in the synthesis of 4-substituted tetrahydroisoquinoline derivatives.

Authors:  Stanimir Manolov; Stoyanka Nikolova; Iliyan Ivanov
Journal:  Molecules       Date:  2013-02-01       Impact factor: 4.411

  10 in total

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