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The best scientist is open to experience and begins with romance - the idea that anything is possible. Ray Bradbury |
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Publications Journal of Medicinal Chemistry DOI: 10.1021/jm201112g Publication Date (Web): December 8, 2011 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 Kinase 2 (JAK2), and Fms-like Tyrosine Kinase-3 (FLT3) for the Treatment of Cancer. Anthony D. William, Angeline C.-H. Lee, Kee Chuan Goh, Stéphanie Blanchard, Anders Poulsen, Ee Ling Teo, Harish Nagaraj, Chai Ping Lee, Haishan Wang, Meredith Williams, Eric T. Sun, Changyong Hu, Ramesh Jayaraman, Mohammed Khalid Pasha, Kantharaj Ethirajulu, Jeanette M. Wood, and Brian W. Dymock. Drug Development - A Case Study Based Insight into Modern Strategies. Edited by: Chris Rundfeldt, ISBN 978-953-307-257-9, Publication date: December 2011 Histone Deacetylase Inhibitors as Therapeutic Agents for Cancer Therapy: Drug Metabolism and Pharmacokinetic Properties. Ethirajulu Kantharaj and Ramesh Jayaraman. Bioorg Med Chem Lett. 2011 Nov 9. Epub ahead of print Structure-based design of PDK1 inhibitors. Poulsen A, Blanchard S, Soh CK, Lee C, Williams M, Wang H, Dymock B. Drug Metab Dispos. 2011 Aug 26. Epub 2011 Aug 26 Preclinical Metabolism and Disposition of SB939(Pracinostat), an Orally Active Histone Deacetylase (HDAC) Inhibitor, and Prediction of Human Pharmacokinetics. Jayaraman R, Pilla Reddy V, Khalid Pasha M, Wang H, Sangthongpitag K, Yeo P, Hu C, Wu X, Xin L, Goh E, New L, Ethirajulu K. Leukemia. 2011 Aug 23. doi: 10.1038/leu.2011.218. TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD, Sun ET, Dymock BW, Ong KH, Ethirajulu K, Burrows F, Wood JM. Leukemia. 2011 Jun 21. doi: 10.1038/leu.2011.148. Epub ahead of print SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Hart S, Goh KC, Novotny-Diermayr V, Hu CY, Hentze H, Tan YC, Madan B, Amalini C, Loh YK, Ong LC, William AD, Lee A, Poulsen A, Jayaraman R, Ong KH, Ethirajulu K, Dymock BW, Wood JW. Journal of Medicinal Chemistry 2011 Jul 14;54(13):4694. Epub 2011 Jun 16. 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. Wang H, Yu N, Chen D, Lee KC, Lye PL, Chang JW, Deng W, Ng MC, Lu T, Khoo ML, Poulsen A, Sangthongpitag K, Wu X, Hu C, Goh KC, Wang X, Fang L, Goh KL, Khng HH, Goh SK, Yeo P, Liu X, Bonday Z, Wood JM, Dymock BW, Kantharaj E, Sun ET. Journal of Medicinal Chemistry 2011 Jul 14;54(13):4638. Epub 2011 Jun 15. 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 for the Treatment of Myelofibrosis and Lymphoma. William AD, Lee AC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Tan E, Chen D, Williams M, Sun ET, Goh KC, Ong WC, Goh SK, Hart S, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW. Molecular Cancer Therapeutics. 2011 Jul;10(7):1207-17. Epub 2011 May 17. Pharmacodynamic Evaluation of the Target Efficacy of SB939, an Oral HDAC Inhibitor with Selectivity for Tumor Tissue. Novotny-Diermayr V, Sausgruber N, Loh YK, Pasha MK, Jayaraman R, Hentze H, Yong WP, Goh BC, Toh HC, Ethirajulu K, Zhu J, Wood JM. Annals of Oncology 2011 Mar 8. Epub ahead of print Phase I and pharmacodynamic study of an orally administered novel inhibitor of histone deacetylases, SB939, in patients with refractory solid malignancies. Yong WP, Goh BC, Soo RA, Toh HC, Ethirajulu K, Wood J, Novotny-Diermayr V, Lee SC, Yeo WL, Chan D, Lim D, Seah E, Lim R, Zhu J. British Journal of Cancer. 2011 Mar 1;104(5):756-62. Epub 2011 Feb 1 Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours. Razak AR, Hotte SJ, Siu LL, Chen EX, Hirte HW, Powers J, Walsh W, Stayner LA, Laughlin A, Novotny-Diermayr V, Zhu J, Eisenhauer EA.
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