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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 (JAK2/FLT3) for the treatment of rheumatoid arthritis.
William AD, Lee AC, Poulsen A, Goh KC, Madan B, Hart S, Tan E, Wang H, Nagaraj H, Chen D, Lee CP, Sun ET, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW. William AD, et al. Among authors: madan b. J Med Chem. 2012 Mar 22;55(6):2623-40. doi: 10.1021/jm201454n. Epub 2012 Mar 6. J Med Chem. 2012. PMID: 22339472
VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
Hart S, Novotny-Diermayr V, Goh KC, Williams M, Tan YC, Ong LC, Cheong A, Ng BK, Amalini C, Madan B, Nagaraj H, Jayaraman R, Pasha KM, Ethirajulu K, Chng WJ, Mustafa N, Goh BC, Benes C, McDermott U, Garnett M, Dymock B, Wood JM. Hart S, et al. Among authors: madan b. Mol Cancer Ther. 2013 Feb;12(2):151-61. doi: 10.1158/1535-7163.MCT-12-0466. Epub 2012 Dec 27. Mol Cancer Ther. 2013. PMID: 23270925 Free PMC article.
Wnt addiction of genetically defined cancers reversed by PORCN inhibition.
Madan B, Ke Z, Harmston N, Ho SY, Frois AO, Alam J, Jeyaraj DA, Pendharkar V, Ghosh K, Virshup IH, Manoharan V, Ong EH, Sangthongpitag K, Hill J, Petretto E, Keller TH, Lee MA, Matter A, Virshup DM. Madan B, et al. Oncogene. 2016 Apr 28;35(17):2197-207. doi: 10.1038/onc.2015.280. Epub 2015 Aug 10. Oncogene. 2016. PMID: 26257057 Free PMC article.
Discovery and Optimization of a Porcupine Inhibitor.
Duraiswamy AJ, Lee MA, Madan B, Ang SH, Tan ES, Cheong WW, Ke Z, Pendharkar V, Ding LJ, Chew YS, Manoharan V, Sangthongpitag K, Alam J, Poulsen A, Ho SY, Virshup DM, Keller TH. Duraiswamy AJ, et al. Among authors: madan b. J Med Chem. 2015 Aug 13;58(15):5889-99. doi: 10.1021/acs.jmedchem.5b00507. Epub 2015 Jul 16. J Med Chem. 2015. PMID: 26110200
Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.
Ho SY, Alam J, Jeyaraj DA, Wang W, Lin GR, Ang SH, Tan ESW, Lee MA, Ke Z, Madan B, Virshup DM, Ding LJ, Manoharan V, Chew YS, Low CB, Pendharkar V, Sangthongpitag K, Hill J, Keller TH, Poulsen A. Ho SY, et al. Among authors: madan b. J Med Chem. 2017 Aug 10;60(15):6678-6692. doi: 10.1021/acs.jmedchem.7b00662. Epub 2017 Jul 20. J Med Chem. 2017. PMID: 28671458
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