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Page 1
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: kohl ne. 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
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beese LS, Beshore DC, Bhimnathwala H, Bogusky MJ, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hamilton KA, Hartman GD, Heimbrook DC, Homnick CF, Huber HE, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Robinson R, Rodrigues AD, Taylor JS, Walsh ES, Williams TM, Zartman CB. Bell IM, et al. Among authors: kohl ne. J Med Chem. 2002 Jun 6;45(12):2388-409. doi: 10.1021/jm010531d. J Med Chem. 2002. PMID: 12036349
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Cox CD, Breslin MJ, Mariano BJ, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Huber HE, Kohl NE, Torrent M, Yan Y, Kuo LC, Hartman GD. Cox CD, et al. Among authors: kohl ne. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2041-5. doi: 10.1016/j.bmcl.2005.02.055. Bioorg Med Chem Lett. 2005. PMID: 15808464
Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP.
Fraley ME, Garbaccio RM, Arrington KL, Hoffman WF, Tasber ES, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Fernandes C, Schaber MD, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Shu C, Torrent M, Heimbrook DC, Kohl NE, Huber HE, Hartman GD. Fraley ME, et al. Among authors: kohl ne. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1775-9. doi: 10.1016/j.bmcl.2006.01.030. Epub 2006 Jan 24. Bioorg Med Chem Lett. 2006. PMID: 16439123
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: kohl ne. 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: kohl ne. 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: kohl ne. 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: kohl ne. 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. 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: kohl ne. 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
111 results