Literature DB >> 20218717

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

Michael E Jung1, Samedy Ouk, Dongwon Yoo, Charles L Sawyers, Charlie Chen, Chris Tran, John Wongvipat.   

Abstract

A structure-activity relationship study was carried out on a series of thiohydantoins and their analogues 14 which led to the discovery of 92 (MDV3100) as the clinical candidate for the treatment of hormone refractory prostate cancer.

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Year:  2010        PMID： 20218717      PMCID： PMC3180999          DOI： 10.1021/jm901488g

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


  12 in total

1.  Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations.

Authors:  P M Matias; P Donner; R Coelho; M Thomaz; C Peixoto; S Macedo; N Otto; S Joschko; P Scholz; A Wegg; S Bäsler; M Schäfer; U Egner; M A Carrondo
Journal:  J Biol Chem       Date:  2000-08-25       Impact factor: 5.157

2.  Homology modeling using multiple molecular dynamics simulations and docking studies of the human androgen receptor ligand binding domain bound to testosterone and nonsteroidal ligands.

Authors:  C A Marhefka; B M Moore; T C Bishop; L Kirkovsky; A Mukherjee; J T Dalton; D D Miller
Journal:  J Med Chem       Date:  2001-05-24       Impact factor: 7.446

3.  Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone.

Authors:  J S Sack; K F Kish; C Wang; R M Attar; S E Kiefer; Y An; G Y Wu; J E Scheffler; M E Salvati; S R Krystek; R Weinmann; H M Einspahr
Journal:  Proc Natl Acad Sci U S A       Date:  2001-04-24       Impact factor: 11.205

4.  Structural basis for antagonism and resistance of bicalutamide in prostate cancer.

Authors:  Casey E Bohl; Wenqing Gao; Duane D Miller; Charles E Bell; James T Dalton
Journal:  Proc Natl Acad Sci U S A       Date:  2005-04-15       Impact factor: 11.205

Review 5.  The development of androgen-independent prostate cancer.

Authors:  B J Feldman; D Feldman
Journal:  Nat Rev Cancer       Date:  2001-10       Impact factor: 60.716

6.  Regulation of growth and epidermal growth factor receptor levels of LNCaP prostate tumor cells by different steroids.

Authors:  A L Schuurmans; J Bolt; M M Voorhorst; R A Blankenstein; E Mulder
Journal:  Int J Cancer       Date:  1988-12-15       Impact factor: 7.396

7.  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

8.  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

Review 9.  Molecular biology of the androgen receptor.

Authors:  Edward P Gelmann
Journal:  J Clin Oncol       Date:  2002-07-01       Impact factor: 44.544

10.  Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor.

Authors:  G Teutsch; F Goubet; T Battmann; A Bonfils; F Bouchoux; E Cerede; D Gofflo; M Gaillard-Kelly; D Philibert
Journal:  J Steroid Biochem Mol Biol       Date:  1994-01       Impact factor: 4.292
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  51 in total

Review 1.  Progress of molecular targeted therapies for prostate cancers.

Authors:  Weihua Fu; Elena Madan; Marla Yee; Hongtao Zhang
Journal:  Biochim Biophys Acta       Date:  2011-11-29

2.  Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.

Authors:  Adegoke O Adeniji; Barry M Twenter; Michael C Byrns; Yi Jin; Mo Chen; Jeffrey D Winkler; Trevor M Penning
Journal:  J Med Chem       Date:  2012-02-15       Impact factor: 7.446

3.  Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer.

Authors:  Mo Chen; Adegoke O Adeniji; Barry M Twenter; Jeffrey D Winkler; David W Christianson; Trevor M Penning
Journal:  Bioorg Med Chem Lett       Date:  2012-03-29       Impact factor: 2.823

4.  Safety and Antitumor Activity of Apalutamide (ARN-509) in Metastatic Castration-Resistant Prostate Cancer with and without Prior Abiraterone Acetate and Prednisone.

Authors:  Dana E Rathkopf; Emmanuel S Antonarakis; Neal D Shore; Ronald F Tutrone; Joshi J Alumkal; Charles J Ryan; Mansoor Saleh; Ralph J Hauke; Rajesh Bandekar; Edna Chow Maneval; Carla J de Boer; Margaret K Yu; Howard I Scher
Journal:  Clin Cancer Res       Date:  2017-02-17       Impact factor: 12.531

5.  Enzalutamide versus flutamide for castration-resistant prostate cancer after combined androgen blockade therapy with bicalutamide: a retrospective study.

Authors:  Taro Iguchi; Satoshi Tamada; Minoru Kato; Sayaka Yasuda; Taiyo Otoshi; Kosuke Hamada; Takeshi Yamasaki; Tatsuya Nakatani
Journal:  Int J Clin Oncol       Date:  2019-02-11       Impact factor: 3.402

6.  The 2011 Gordon Wilson Lecture: overcoming resistance to targeted cancer drugs.

Authors:  Charles L Sawyers
Journal:  Trans Am Clin Climatol Assoc       Date:  2012

Review 7.  New agents in the arsenal to fight castrate-resistant prostate cancer.

Authors:  Erin E Ezzell; Kuang S Chang; Benjamin J George
Journal:  Curr Oncol Rep       Date:  2013-06       Impact factor: 5.075

8.  Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators.

Authors:  Antonella Pepe; Michael Pamment; Yeong Sang Kim; Sunmin Lee; Min-Jung Lee; Kristin Beebe; Anton Filikov; Len Neckers; Jane B Trepel; Sanjay V Malhotra
Journal:  J Med Chem       Date:  2013-10-30       Impact factor: 7.446

9.  CUDC-101, a Novel Inhibitor of Full-Length Androgen Receptor (flAR) and Androgen Receptor Variant 7 (AR-V7) Activity: Mechanism of Action and In Vivo Efficacy.

Authors:  Huiying Sun; Sanjay N Mediwala; Adam T Szafran; Michael A Mancini; Marco Marcelli
Journal:  Horm Cancer       Date:  2016-03-08       Impact factor: 3.869

10.  Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.

Authors:  Puranik Purushottamachar; Abhijit M Godbole; Lalji K Gediya; Marlena S Martin; Tadas S Vasaitis; Andrew K Kwegyir-Afful; Senthilmurugan Ramalingam; Zeynep Ates-Alagoz; Vincent C O Njar
Journal:  J Med Chem       Date:  2013-06-07       Impact factor: 7.446
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