Wei Sheng Huang

Summary

Affiliation: ARIAD Pharmaceuticals
Country: USA

Publications

  1. doi request reprint 9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation
    Wei Sheng Huang
    ARIAD Pharmaceuticals, Inc, 26 Landsdowne Street, Cambridge, Massachusetts 02139, USA
    J Med Chem 52:4743-56. 2009
  2. doi request reprint Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th
    Wei Sheng Huang
    ARIAD Pharmaceuticals, Inc, 26 Landsdowne Street, Cambridge, Massachusetts 02139, USA
    J Med Chem 53:4701-19. 2010
  3. doi request reprint Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance
    Tianjun Zhou
    ARIAD Pharmaceuticals Inc, 26 Landsdowne Street, Cambridge, MA 02139, USA
    Chem Biol Drug Des 77:1-11. 2011
  4. doi request reprint Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors
    Yihan Wang
    ARIAD Pharmaceuticals, Inc, 26 Landsdowne Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 18:4907-12. 2008
  5. doi request reprint Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template
    Tianjun Zhou
    ARIAD Pharmaceuticals Inc, 26 Landsdowne St, Cambridge, MA 02139, USA
    Chem Biol Drug Des 75:18-28. 2010
  6. doi request reprint Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant
    Mathew Thomas
    ARIAD Pharmaceuticals Inc, 26 Lansdowne Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 21:3743-8. 2011
  7. doi request reprint Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors
    Anna Kohlmann
    ARIAD Pharmaceuticals, Inc, 26 Landsdowne Street, Cambridge, Massachusetts 02139, USA
    J Med Chem 56:1023-40. 2013
  8. ncbi request reprint Catalytic asymmetric reductive coupling of alkynes and aldehydes: enantioselective synthesis of allylic alcohols and alpha-hydroxy ketones
    Karen M Miller
    Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA
    J Am Chem Soc 125:3442-3. 2003

Collaborators

Detail Information

Publications8

  1. doi request reprint 9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation
    Wei Sheng Huang
    ARIAD Pharmaceuticals, Inc, 26 Landsdowne Street, Cambridge, Massachusetts 02139, USA
    J Med Chem 52:4743-56. 2009
    ..Notably, several inhibitors (e.g., 14a, AP24163) exhibited modest cellular potency (IC50 = 300-400 nM) against the Bcr-Abl mutant T315I, a variant resistant to all currently marketed therapies for chronic myeloid leukemia...
  2. doi request reprint Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th
    Wei Sheng Huang
    ARIAD Pharmaceuticals, Inc, 26 Landsdowne Street, Cambridge, Massachusetts 02139, USA
    J Med Chem 53:4701-19. 2010
    ..These data, coupled with a favorable ADME profile, support the potential of 20g to be an effective treatment for CML, including patients refractory to all currently approved therapies...
  3. doi request reprint Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance
    Tianjun Zhou
    ARIAD Pharmaceuticals Inc, 26 Landsdowne Street, Cambridge, MA 02139, USA
    Chem Biol Drug Des 77:1-11. 2011
    ..The inhibitory mechanism exemplified by ponatinib may have broad relevance to designing inhibitors against other kinases with mutated gatekeeper residues...
  4. doi request reprint Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors
    Yihan Wang
    ARIAD Pharmaceuticals, Inc, 26 Landsdowne Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 18:4907-12. 2008
    ..Most compounds are potent inhibitors of both Src and Abl kinase, and several possess good oral bioavailability...
  5. doi request reprint Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template
    Tianjun Zhou
    ARIAD Pharmaceuticals Inc, 26 Landsdowne St, Cambridge, MA 02139, USA
    Chem Biol Drug Des 75:18-28. 2010
    ..The data presented here provides structural guidance for the further design of novel potent DFG-out class inhibitors against Src, Abl and Abl T315I mutant kinases...
  6. doi request reprint Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant
    Mathew Thomas
    ARIAD Pharmaceuticals Inc, 26 Lansdowne Street, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 21:3743-8. 2011
    ..Several compounds in this series displayed excellent in vitro potency against both native BCR-ABL and the T315I mutant. Notably, a subset of inhibitors exhibited desirable PK and were orally active in a mouse model of T315I-driven CML...
  7. doi request reprint Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors
    Anna Kohlmann
    ARIAD Pharmaceuticals, Inc, 26 Landsdowne Street, Cambridge, Massachusetts 02139, USA
    J Med Chem 56:1023-40. 2013
    ..Selected molecules inhibited lactate production in cells, suggesting target-specific inhibition in cancer cell lines...
  8. ncbi request reprint Catalytic asymmetric reductive coupling of alkynes and aldehydes: enantioselective synthesis of allylic alcohols and alpha-hydroxy ketones
    Karen M Miller
    Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA
    J Am Chem Soc 125:3442-3. 2003
    ..In conjunction with ozonolysis, this process is complementary to existing methods of enantioselective alpha-hydroxy ketone synthesis...