Literature DB >> 24900495

Nonsteroidal androgen receptor ligands: versatile syntheses and biological data.

Greta Varchi1, Andrea Guerrini1, Anna Tesei2, Giovanni Brigliadori2, Carlo Bertucci3, Marzia Di Donato4, Gabriella Castoria4.   

Abstract

We report herein a stereoselective and straightforward methodology for the synthesis of new androgen receptor ligands with (anti)-agonistic activities. Oxygen-nitrogen replacement in bicalutamide-like structures paves the way to the disclosure of a new class of analogues, including cyclized/nitrogen-substituted derivatives, with promising antiandrogen (or anabolic) activity.

Entities:  

Keywords:  androgen receptor; enantiopure antiandrogens; hormone-refractory prostate cancer; sulfinylimino propanamides

Year:  2012        PMID： 24900495      PMCID： PMC4025740          DOI： 10.1021/ml3000269

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  21 in total

1.  Asymmetric synthesis of new chiral N-sulfinyl 2,2-disubstituted aziridines by Grignard additions across alpha-chloro N-sulfinyl ketimines.

Authors:  Filip Colpaert; Sven Mangelinckx; Erika Leemans; Bram Denolf; Norbert De Kimpe
Journal:  Org Biomol Chem       Date:  2010-05-25       Impact factor: 3.876

2.  Highly diastereoselective synthesis of α-difluoromethyl amines from N-tert-butylsulfinyl ketimines and difluoromethyl phenyl sulfone.

Authors:  Jun Liu; Jinbo Hu
Journal:  Chemistry       Date:  2010-10-04       Impact factor: 5.236

3.  Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).

Authors:  Michael E Jung; Samedy Ouk; Dongwon Yoo; Charles L Sawyers; Charlie Chen; Chris Tran; John Wongvipat
Journal:  J Med Chem       Date:  2010-04-08       Impact factor: 7.446

Review 4.  The androgen receptor in LNCaP cells contains a mutation in the ligand binding domain which affects steroid binding characteristics and response to antiandrogens.

Authors:  J Veldscholte; C A Berrevoets; C Ris-Stalpers; G G Kuiper; G Jenster; J Trapman; A O Brinkmann; E Mulder
Journal:  J Steroid Biochem Mol Biol       Date:  1992-03       Impact factor: 4.292

5.  Prostate specific antigen decreases after withdrawal of antiandrogen therapy with bicalutamide or flutamide in patients receiving combined androgen blockade.

Authors:  P F Schellhammer; P Venner; G P Haas; E J Small; P T Nieh; D R Seabaugh; A L Patterson; E Klein; Z Wajsman; B Furr; Y Chen; G J Kolvenbag
Journal:  J Urol       Date:  1997-05       Impact factor: 7.450

6.  Androgen-induced cell migration: role of androgen receptor/filamin A association.

Authors:  Gabriella Castoria; Loredana D'Amato; Alessandra Ciociola; Pia Giovannelli; Tiziana Giraldi; Leandra Sepe; Giovanni Paolella; Maria Vittoria Barone; Antimo Migliaccio; Ferdinando Auricchio
Journal:  PLoS One       Date:  2011-02-16       Impact factor: 3.240

7.  New colorimetric cytotoxicity assay for anticancer-drug screening.

Authors:  P Skehan; R Storeng; D Scudiero; A Monks; J McMahon; D Vistica; J T Warren; H Bokesch; S Kenney; M R Boyd
Journal:  J Natl Cancer Inst       Date:  1990-07-04       Impact factor: 13.506

Review 8.  Androgen replacement therapy: present and future.

Authors:  Louis J G Gooren; Mathijs C M Bunck
Journal:  Drugs       Date:  2004       Impact factor: 9.546

9.  Development of a second-generation antiandrogen for treatment of advanced prostate cancer.

Authors:  Chris Tran; Samedy Ouk; Nicola J Clegg; Yu Chen; Philip A Watson; Vivek Arora; John Wongvipat; Peter M Smith-Jones; Dongwon Yoo; Andrew Kwon; Teresa Wasielewska; Derek Welsbie; Charlie Degui Chen; Celestia S Higano; Tomasz M Beer; David T Hung; Howard I Scher; Michael E Jung; Charles L Sawyers
Journal:  Science       Date:  2009-04-09       Impact factor: 47.728

10.  Molecular determinants of resistance to antiandrogen therapy.

Authors:  Charlie D Chen; Derek S Welsbie; Chris Tran; Sung Hee Baek; Randy Chen; Robert Vessella; Michael G Rosenfeld; Charles L Sawyers
Journal:  Nat Med       Date:  2003-12-21       Impact factor: 53.440
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  1 in total

1.  Seviteronel, a Novel CYP17 Lyase Inhibitor and Androgen Receptor Antagonist, Radiosensitizes AR-Positive Triple Negative Breast Cancer Cells.

Authors:  Anna R Michmerhuizen; Benjamin Chandler; Eric Olsen; Kari Wilder-Romans; Leah Moubadder; Meilan Liu; Andrea M Pesch; Amanda Zhang; Cassandra Ritter; S Tanner Ward; Alyssa Santola; Shyam Nyati; James M Rae; Daniel Hayes; Felix Y Feng; Daniel Spratt; Daniel Wahl; Joel Eisner; Lori J Pierce; Corey Speers
Journal:  Front Endocrinol (Lausanne)       Date:  2020-02-11       Impact factor: 5.555
  1 in total

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