Literature DB >> 17703938

Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.

Robert I Higuchi1, Anthony W Thompson, Jyun-Hung Chen, Thomas R Caferro, Marquis L Cummings, Charlotte P Deckhut, Mark E Adams, Christopher M Tegley, James P Edwards, Francisco J López, E Adam Kallel, Donald S Karanewsky, William T Schrader, Keith B Marschke, Lin Zhi.   

Abstract

A series of androgen receptor modulators based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones was synthesized and evaluated in an androgen receptor transcriptional activation assay. The most potent analogues from the series exhibited single-digit nanomolar potency in vitro. Compound 18h demonstrated full efficacy in the maintenance of muscle weight, at 10 mg/kg, with reduced activity in prostate weight in an in vivo model of androgen action.

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Year:  2007        PMID： 17703938      PMCID： PMC2739385          DOI： 10.1016/j.bmcl.2007.07.034

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


  15 in total

Review 1.  Selective androgen receptor modulators (SARMs): a novel approach to androgen therapy for the new millennium.

Authors:  A Negro-Vilar
Journal:  J Clin Endocrinol Metab       Date:  1999-10       Impact factor: 5.958

2.  Myotrophic activity of 19-nortestosterone and other steroids determined by modified levator ani muscle method.

Authors:  L G HERSHBERGER; E G SHIPLEY; R K MEYER
Journal:  Proc Soc Exp Biol Med       Date:  1953-05

3.  Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators.

Authors:  Xuqing Zhang; George F Allan; Tifanie Sbriscia; Olivia Linton; Scott G Lundeen; Zhihua Sui
Journal:  Bioorg Med Chem Lett       Date:  2006-09-07       Impact factor: 2.823

4.  Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.

Authors:  Arjan van Oeveren; Mehrnouch Motamedi; Neelakandha S Mani; Keith B Marschke; Francisco J López; William T Schrader; Andrés Negro-Vilar; Lin Zhi
Journal:  J Med Chem       Date:  2006-10-19       Impact factor: 7.446

5.  Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.

Authors:  L G Hamann; R I Higuchi; L Zhi; J P Edwards; X N Wang; K B Marschke; J W Kong; L J Farmer; T K Jones
Journal:  J Med Chem       Date:  1998-02-12       Impact factor: 7.446

Review 6.  Androgens in men--uses and abuses.

Authors:  C J Bagatell; W J Bremner
Journal:  N Engl J Med       Date:  1996-03-14       Impact factor: 91.245

Review 7.  Intracellular receptors and signal transducers and activators of transcription superfamilies: novel targets for small-molecule drug discovery.

Authors:  J Rosen; A Day; T K Jones; E T Jones; A M Nadzan; R B Stein
Journal:  J Med Chem       Date:  1995-12-08       Impact factor: 7.446

8.  Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.

Authors:  Chongqing Sun; Jeffrey A Robl; Tammy C Wang; Yanting Huang; Joyce E Kuhns; John A Lupisella; Blake C Beehler; Rajasree Golla; Paul G Sleph; Ramakrishna Seethala; Aberra Fura; Stanley R Krystek; Yongmi An; Mary F Malley; John S Sack; Mark E Salvati; Gary J Grover; Jacek Ostrowski; Lawrence G Hamann
Journal:  J Med Chem       Date:  2006-12-28       Impact factor: 7.446

9.  Older men are as responsive as young men to the anabolic effects of graded doses of testosterone on the skeletal muscle.

Authors:  Shalender Bhasin; Linda Woodhouse; Richard Casaburi; Atam B Singh; Ricky Phong Mac; Martin Lee; Kevin E Yarasheski; Indrani Sinha-Hikim; Connie Dzekov; Jeanne Dzekov; Lynne Magliano; Thomas W Storer
Journal:  J Clin Endocrinol Metab       Date:  2004-11-23       Impact factor: 5.958

10.  Testosterone replacement increases fat-free mass and muscle size in hypogonadal men.

Authors:  S Bhasin; T W Storer; N Berman; K E Yarasheski; B Clevenger; J Phillips; W P Lee; T J Bunnell; R Casaburi
Journal:  J Clin Endocrinol Metab       Date:  1997-02       Impact factor: 5.958
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  1 in total

Review 1.  Selective androgen receptor modulators in preclinical and clinical development.

Authors:  Ramesh Narayanan; Michael L Mohler; Casey E Bohl; Duane D Miller; James T Dalton
Journal:  Nucl Recept Signal       Date:  2008-11-26
  1 in total

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