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Page 1
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors.
Converso A, Hartingh T, Garbaccio RM, Tasber E, Rickert K, Fraley ME, Yan Y, Kreatsoulas C, Stirdivant S, Drakas B, Walsh ES, Hamilton K, Buser CA, Mao X, Abrams MT, Beck SC, Tao W, Lobell R, Sepp-Lorenzino L, Zugay-Murphy J, Sardana V, Munshi SK, Jezequel-Sur SM, Zuck PD, Hartman GD. Converso A, et al. Among authors: tao w. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1240-4. doi: 10.1016/j.bmcl.2008.12.076. Epub 2008 Dec 24. Bioorg Med Chem Lett. 2009. PMID: 19155174
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: tao w. 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 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: tao w. 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: tao w. 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
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.
Fraley ME, Steen JT, Brnardic EJ, Arrington KL, Spencer KL, Hanney BA, Kim Y, Hartman GD, Stirdivant SM, Drakas BA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L, Yan Y, Ikuta M, Munshi SK, Kuo LC, Kreatsoulas C. Fraley ME, et al. Among authors: tao w. Bioorg Med Chem Lett. 2006 Dec 1;16(23):6049-53. doi: 10.1016/j.bmcl.2006.08.118. Epub 2006 Sep 15. Bioorg Med Chem Lett. 2006. PMID: 16978863
Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors.
Huang S, Garbaccio RM, Fraley ME, Steen J, Kreatsoulas C, Hartman G, Stirdivant S, Drakas B, Rickert K, Walsh E, Hamilton K, Buser CA, Hardwick J, Mao X, Abrams M, Beck S, Tao W, Lobell R, Sepp-Lorenzino L, Yan Y, Ikuta M, Murphy JZ, Sardana V, Munshi S, Kuo L, Reilly M, Mahan E. Huang S, et al. Among authors: tao w. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5907-12. doi: 10.1016/j.bmcl.2006.08.053. Epub 2006 Sep 20. Bioorg Med Chem Lett. 2006. PMID: 16990002
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: tao w. 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: tao w. 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: tao w. 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
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
Brnardic EJ, Garbaccio RM, Fraley ME, Tasber ES, Steen JT, Arrington KL, Dudkin VY, Hartman GD, Stirdivant SM, Drakas BA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L, Yan Y, Ikuta M, Munshi SK, Kuo LC, Kreatsoulas C. Brnardic EJ, et al. Among authors: tao w. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5989-94. doi: 10.1016/j.bmcl.2007.07.051. Epub 2007 Aug 19. Bioorg Med Chem Lett. 2007. PMID: 17804227
2,738 results