Stéphanie Blanchard

Summary

Publications

  1. doi 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
  2. doi Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors
    Stéphanie Blanchard
    S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 20:2443-7. 2010
  3. doi Structure-based design of oxygen-linked macrocyclic kinase inhibitors: discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3)
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore, 117 528, Singapore
    J Comput Aided Mol Des 26:437-50. 2012
  4. doi Thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening
    Angeline C H Lee
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 22:4023-7. 2012
  5. doi 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. doi Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3)
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore, 117 528, Singapore
    J Mol Model 19:119-30. 2013
  7. doi 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
  8. doi Structure-based design of Aurora A & B inhibitors
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, 117 528, Singapore, Singapore
    J Comput Aided Mol Des 22:897-906. 2008
  9. doi Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor
    Anthony D William
    S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore
    J Med Chem 54:4638-58. 2011

Collaborators

  • Haishan Wang
  • Anders Poulsen
  • Kee Chuan Goh
  • Meredith Williams
  • Harish Nagaraj
  • Angeline C H Lee
  • Anthony D William
  • Evelyn Tan
  • Brian Dymock
  • Ee Ling Teo
  • Brian W Dymock
  • Anthony William
  • Angeline Lee
  • Jeanette M Wood
  • Eric T Sun
  • Mohammed Khalid Pasha
  • Ramesh Jayaraman
  • Kantharaj Ethirajulu
  • Eric Sun
  • Kay Lin Goh
  • Zahid Bonday
  • Eeling Teo
  • Wai Chung Ong
  • Chang Kai Soh
  • Changyong Hu
  • Chaiping Lee
  • Jeanette Wood
  • Miah Kiat Goh
  • Pondy Murugappan Ramanujulu
  • Chai Ping Lee
  • Diana M Ma
  • Dizhong Chen
  • Siok Kun Goh
  • Stefan Hart
  • Weiping Deng
  • Noah Tu
  • Chee Pang Ng

Detail Information

Publications9

  1. doi 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...
  2. doi Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors
    Stéphanie Blanchard
    S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 20:2443-7. 2010
    ..Several promising leads were optimized for selectivity towards Aurora B. Excellent binding affinity and good selectivity were achieved with optimized compounds in isolated Aurora subfamily assays...
  3. doi Structure-based design of oxygen-linked macrocyclic kinase inhibitors: discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3)
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore, 117 528, Singapore
    J Comput Aided Mol Des 26:437-50. 2012
    ..Another selective JAK2/FLT3 inhibitor, 33 (SB1578), has entered phase 1 clinical development for the non-oncology indication rheumatoid arthritis...
  4. doi Thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening
    Angeline C H Lee
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
    Bioorg Med Chem Lett 22:4023-7. 2012
    ....
  5. doi 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. doi Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3)
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, Singapore, 117 528, Singapore
    J Mol Model 19:119-30. 2013
    ..Compound 5 (SB1317/TG02), a pan-CDK/FLT3/JAK2 inhibitor, was selected for preclinical development, and is now in phase 1 clinical trials...
  7. doi 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...
  8. doi Structure-based design of Aurora A & B inhibitors
    Anders Poulsen
    S BIO Pte Ltd, 1 Science Park Road, 05 09 The Capricorn, Singapore Science Park II, 117 528, Singapore, Singapore
    J Comput Aided Mol Des 22:897-906. 2008
    ..Finally we calculate the conformational energy penalty of the putative bioactive conformation of our inhibitors and show that this property correlates well with the Aurora A binding affinity...
  9. doi Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor
    Anthony D William
    S BIO Pte Ltd, The Capricorn, Singapore Science Park II, Singapore
    J Med Chem 54:4638-58. 2011
    ..Compound 21c (SB1518) was selected as a development candidate and progressed into clinical trials where it is currently in phase 2 for MF and lymphoma...