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Page 1
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: buser ca. J Med Chem. 2002 Jun 6;45(12):2388-409. doi: 10.1021/jm010531d. J Med Chem. 2002. PMID: 12036349
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Nguyen DN, Stump CA, Walsh ES, Fernandes C, Davide JP, Ellis-Hutchings M, Robinson RG, Williams TM, Lobell RB, Huber HE, Buser CA. Nguyen DN, et al. Among authors: buser ca. Bioorg Med Chem Lett. 2002 May 6;12(9):1269-73. doi: 10.1016/s0960-894x(02)00154-3. Bioorg Med Chem Lett. 2002. PMID: 11965368
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Tucker TJ, Abrams MT, Buser CA, Davide JP, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Huber HE, Liu D, Lobell RB, Lumma WC, Robinson RG, Sisko JT, Smith AM. Tucker TJ, et al. Among authors: buser ca. Bioorg Med Chem Lett. 2002 Aug 5;12(15):2027-30. doi: 10.1016/s0960-894x(02)00308-6. Bioorg Med Chem Lett. 2002. PMID: 12113834
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Fraley ME, Arrington KL, Buser CA, Ciecko PA, Coll KE, Fernandes C, Hartman GD, Hoffman WF, Lynch JJ, McFall RC, Rickert K, Singh R, Smith S, Thomas KA, Wong BK. Fraley ME, et al. Among authors: buser ca. Bioorg Med Chem Lett. 2004 Jan 19;14(2):351-5. doi: 10.1016/j.bmcl.2003.11.007. Bioorg Med Chem Lett. 2004. PMID: 14698157
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Dinsmore CJ, Zartman CB, Bergman JM, Abrams MT, Buser CA, Culberson JC, Davide JP, Ellis-Hutchings M, Fernandes C, Graham SL, Hartman GD, Huber HE, Lobell RB, Mosser SD, Robinson RG, Williams TM. Dinsmore CJ, et al. Among authors: buser ca. Bioorg Med Chem Lett. 2004 Feb 9;14(3):639-43. doi: 10.1016/j.bmcl.2003.11.051. Bioorg Med Chem Lett. 2004. PMID: 14741259
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: buser ca. 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 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: buser ca. 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: buser ca. 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: buser ca. 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
58 results