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      A New Generation of Selective Androgen Receptor Degraders : Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity

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      SARD_Manuscript_jm_2018_00973e._R3_12.7.2018.pdf (1.979Mb)
      Publication date
      2019
      Author
      Hwang, Dong-Jin
      He, Yali
      Ponnusamy, Suriyan
      Mohler, Michael L.
      Thiyagarajan, Thirumagal
      McEwan, Iain J.
      Narayanan, Ramesh
      Miller, Duane D.
      Keywords
      SDG 3 - Good Health and Well-being
      structure-activity relationship
      selective androgen receptor degrader
      androgen receptor
      androgen receptor splice variant
      AR-V7
      AR escape mutants
      Antagonist
      prostate cancer
      Antiandrogen resistance
      Enzalutamide resistance
      Castration-resistant prostate cancer
      N-terminal domain
      Ligand binding domain
      Prostate-specific antigen
      AR activation function domain-1
      R Medicine (General)
      Drug Discovery
      Molecular Medicine
      Supplementary Data
      supplementary data available
      Metadata
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      Citation
      Hwang , D-J , He , Y , Ponnusamy , S , Mohler , M L , Thiyagarajan , T , McEwan , I J , Narayanan , R & Miller , D D 2019 , ' A New Generation of Selective Androgen Receptor Degraders : Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity ' , Journal of Medicinal Chemistry , vol. 62 , no. 2 , pp. 491-511 . https://doi.org/10.1021/acs.jmedchem.8b00973
      Publication
      Journal of Medicinal Chemistry
      Status
      Peer reviewed
      DOI
      https://doi.org/https://doi.org/10.1021/acs.jmedchem.8b00973
      ISSN
      0022-2623
      Type
      Journal article
      Description
      This research was supported by the Van Vleet Endowed Professorship (D.D.M.), and GTx, Inc. grant (R.N. and D.D.M.) We thank GTx, Inc. for supporting this project and Dr. Dejian Ma of UTHSC, College of Pharmacy for assistance with 2D NMR and HRMS experiments.
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      URL
      http://www.scopus.com/inward/record.url?scp=85059636744&partnerID=8YFLogxK
      http://www.mendeley.com/research/new-generation-selective-androgen-receptor-degraders-initial-design-synthesis-biological-evaluation
      URI
      https://hdl.handle.net/2164/13357

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