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Page 1
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Garbaccio RM, Tasber ES, Neilson LA, Coleman PJ, Fraley ME, Olson C, Bergman J, Torrent M, Buser CA, Rickert K, Walsh ES, Hamilton K, Lobell RB, Tao W, South VJ, Diehl RE, Davide JP, Yan Y, Kuo LC, Li C, Prueksaritanont T, Fernandez-Metzler C, Mahan EA, Slaughter DE, Salata JJ, Kohl NE, Huber HE, Hartman GD. Garbaccio RM, et al. Among authors: south vj. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5671-6. doi: 10.1016/j.bmcl.2007.07.067. Epub 2007 Aug 21. Bioorg Med Chem Lett. 2007. PMID: 17804233
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Garbaccio RM, Fraley ME, Tasber ES, Olson CM, Hoffman WF, Arrington KL, Torrent M, Buser CA, Walsh ES, Hamilton K, Schaber MD, Fernandes C, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Slaughter DE, Shu C, Heimbrook DC, Kohl NE, Huber HE, Hartman GD. Garbaccio RM, et al. Among authors: south vj. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1780-3. doi: 10.1016/j.bmcl.2005.12.094. Epub 2006 Jan 24. Bioorg Med Chem Lett. 2006. PMID: 16439122
Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.
Cox CD, Torrent M, Breslin MJ, Mariano BJ, Whitman DB, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Schaber MD, Lobell RB, Tao W, South VJ, Kohl NE, Yan Y, Kuo LC, Prueksaritanont T, Slaughter DE, Li C, Mahan E, Lu B, Hartman GD. Cox CD, et al. Among authors: south vj. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3175-9. doi: 10.1016/j.bmcl.2006.03.040. Epub 2006 Apr 5. Bioorg Med Chem Lett. 2006. PMID: 16603356
Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.
Cox CD, Breslin MJ, Whitman DB, Coleman PJ, Garbaccio RM, Fraley ME, Zrada MM, Buser CA, Walsh ES, Hamilton K, Lobell RB, Tao W, Abrams MT, South VJ, Huber HE, Kohl NE, Hartman GD. Cox CD, et al. Among authors: south vj. Bioorg Med Chem Lett. 2007 May 15;17(10):2697-702. doi: 10.1016/j.bmcl.2007.03.006. Epub 2007 Mar 6. Bioorg Med Chem Lett. 2007. PMID: 17395460
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.
Coleman PJ, Schreier JD, Cox CD, Fraley ME, Garbaccio RM, Buser CA, Walsh ES, Hamilton K, Lobell RB, Rickert K, Tao W, Diehl RE, South VJ, Davide JP, Kohl NE, Yan Y, Kuo L, Prueksaritanont T, Li C, Mahan EA, Fernandez-Metzler C, Salata JJ, Hartman GD. Coleman PJ, et al. Among authors: south vj. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5390-5. doi: 10.1016/j.bmcl.2007.07.046. Epub 2007 Aug 6. Bioorg Med Chem Lett. 2007. PMID: 17761419
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.
Roecker AJ, Coleman PJ, Mercer SP, Schreier JD, Buser CA, Walsh ES, Hamilton K, Lobell RB, Tao W, Diehl RE, South VJ, Davide JP, Kohl NE, Yan Y, Kuo LC, Li C, Fernandez-Metzler C, Mahan EA, Prueksaritanont T, Hartman GD. Roecker AJ, et al. Among authors: south vj. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5677-82. doi: 10.1016/j.bmcl.2007.07.074. Epub 2007 Aug 21. Bioorg Med Chem Lett. 2007. PMID: 17766111
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
Cox CD, Coleman PJ, Breslin MJ, Whitman DB, Garbaccio RM, Fraley ME, Buser CA, Walsh ES, Hamilton K, Schaber MD, Lobell RB, Tao W, Davide JP, Diehl RE, Abrams MT, South VJ, Huber HE, Torrent M, Prueksaritanont T, Li C, Slaughter DE, Mahan E, Fernandez-Metzler C, Yan Y, Kuo LC, Kohl NE, Hartman GD. Cox CD, et al. Among authors: south vj. J Med Chem. 2008 Jul 24;51(14):4239-52. doi: 10.1021/jm800386y. Epub 2008 Jun 25. J Med Chem. 2008. PMID: 18578472
15 results