Haishan Wang

Summary

Publications

  1. ncbi New patented histone deacetylase inhibitors
    Haishan Wang
    Chemistry Discovery, S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore, Singapore
    Expert Opin Ther Pat 19:1727-57. 2009
  2. ncbi Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity
    Haishan Wang
    Department of Chemistry Discovery, S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 20:3314-21. 2010
  3. ncbi Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile
    Haishan Wang
    Chemistry Discovery, S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore, Singapore
    J Med Chem 54:4694-720. 2011
  4. ncbi N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity
    Haishan Wang
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 19:1403-8. 2009
  5. ncbi Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus k
    Anthony D William
    S BIO Pte Ltd, 1 Science Park Road, No 05 09, The Capricorn, Singapore Science Park II, 117528, Singapore
    J Med Chem 55:169-96. 2012
  6. ncbi SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer
    Veronica Novotny-Diermayr
    S BIO Pte Ltd, 05 09 The Capricorn, Singapore Science Park II, Singapore
    Mol Cancer Ther 9:642-52. 2010
  7. ncbi Preclinical metabolism and disposition of SB939 (Pracinostat), an orally active histone deacetylase inhibitor, and prediction of human pharmacokinetics
    Ramesh Jayaraman
    S BIO Pte Ltd, 1 Science Park Road, No 05 09, The Capricorn, Singapore Science Park II, Singapore 117528
    Drug Metab Dispos 39:2219-32. 2011
  8. ncbi Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK
    Anthony D William
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528
    J Med Chem 55:2623-40. 2012
  9. ncbi 2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1
    Stéphanie Blanchard
    S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore, Singapore
    Bioorg Med Chem Lett 22:2880-4. 2012
  10. ncbi Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 22:1009-13. 2012

Collaborators

  • Stéphanie Blanchard
  • Brian Dymock
  • Michael Entzeroth
  • Niefang Yu
  • Xin Liu
  • Hannes Hentze
  • Veronica Novotny-Diermayr
  • Anders Poulsen
  • Anthony D William
  • Ramesh Jayaraman
  • Meredith Williams
  • Kantharaj Ethirajulu
  • Kee Chuan Goh
  • Chang Kai Soh
  • Harish Nagaraj
  • Eric T Sun
  • Angeline C H Lee
  • Chai Ping Lee
  • Jeanette M Wood
  • Mohammed Khalid Pasha
  • Vasantha M Nayagam
  • Harish Mysore Nagaraj
  • Changyong Hu
  • Evelyn Tan
  • Ee Ling Teo
  • Stefan Hart
  • Dizhong Chen
  • Babita Madan
  • Mohammad Khalid Pasha
  • Zheng Chang Xiong
  • Chaiping Lee
  • Evelyn Goh
  • Chang Yong Hu
  • Lee Sun New
  • Liu Xin
  • Xiaofeng Wu
  • Pauline Yeo
  • Venkatesh Pilla Reddy
  • Kanda Sangthongpitag
  • Walter Stünkel
  • Xukun Wang
  • Binhui Ni
  • Yong Cheng Tan
  • Tony Ng
  • Hong Yan Song

Detail Information

Publications12

  1. ncbi New patented histone deacetylase inhibitors
    Haishan Wang
    Chemistry Discovery, S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore, Singapore
    Expert Opin Ther Pat 19:1727-57. 2009
    ..Given the breadth and depth of recent reporting of novel HDACis, there has emerged a need to review the field from a chemist's perspective in one compact article...
  2. ncbi Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity
    Haishan Wang
    Department of Chemistry Discovery, S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 20:3314-21. 2010
    ....
  3. ncbi Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile
    Haishan Wang
    Chemistry Discovery, S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore, Singapore
    J Med Chem 54:4694-720. 2011
    ..When orally dosed to tumor-bearing mice, 3 is enriched in tumor tissue which may contribute to its potent antitumor activity and prolonged duration of action. 3 is currently being tested in phase I and phase II clinical trials...
  4. ncbi N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity
    Haishan Wang
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 19:1403-8. 2009
    ..Optimized compounds are much more potent than SAHA in both enzymatic and cellular assays. A representative compound, 23 (SB639), has demonstrated antitumor activity in a colon cancer xenograft model...
  5. ncbi Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus k
    Anthony D William
    S BIO Pte Ltd, 1 Science Park Road, No 05 09, The Capricorn, Singapore Science Park II, 117528, Singapore
    J Med Chem 55:169-96. 2012
    ..26h (SB1317/TG02) was progressed into development in 2010 and is currently undergoing phase 1 clinical trials in advanced leukemias and multiple myeloma...
  6. ncbi SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer
    Veronica Novotny-Diermayr
    S BIO Pte Ltd, 05 09 The Capricorn, Singapore Science Park II, Singapore
    Mol Cancer Ther 9:642-52. 2010
    ..The efficacy of SB939 reported here in two very different models of colorectal cancer warrants further investigation in patients...
  7. ncbi Preclinical metabolism and disposition of SB939 (Pracinostat), an orally active histone deacetylase inhibitor, and prediction of human pharmacokinetics
    Ramesh Jayaraman
    S BIO Pte Ltd, 1 Science Park Road, No 05 09, The Capricorn, Singapore Science Park II, Singapore 117528
    Drug Metab Dispos 39:2219-32. 2011
    ..Simcyp predictions showed lack of CYP3A4 and 2C19 drug-drug interaction potential for SB939. In summary, the preclinical ADME of SB939 supported its preclinical and clinical development as an oral drug candidate...
  8. ncbi Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK
    Anthony D William
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528
    J Med Chem 55:2623-40. 2012
    ..Compound 14l (SB1578) was progressed into development and is currently undergoing phase 1 clinical trials in healthy volunteers...
  9. ncbi 2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1
    Stéphanie Blanchard
    S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore, Singapore
    Bioorg Med Chem Lett 22:2880-4. 2012
    ..The synthesis, SAR and ADME properties of this series of compounds are discussed culminating in the discovery of compound 6 which possessed sub-micromolar cell proliferation activity and 65% oral bioavailability in mice...
  10. ncbi Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 22:1009-13. 2012
    ..Exploiting shape differences in the binding-site allowed for the design of mTOR selective inhibitors. Focus on ligand efficiency ensured the inhibitors retained a low molecular weight and desirable drug-like properties...
  11. ncbi Structure-based design of PDK1 inhibitors
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 22:305-7. 2012
    ..This improved both binding to the enzyme and physiochemical properties without compromising ligand efficiency...
  12. ncbi SIRT1 modulating compounds from high-throughput screening as anti-inflammatory and insulin-sensitizing agents
    Vasantha M Nayagam
    S BIO Pte Ltd, Singapore
    J Biomol Screen 11:959-67. 2006
    ..In contrast, a SIRT1 inhibitory compound showed a stimulatory activity on the differentiation of adipocytes, a feature often linked to insulin sensitization...