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From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.
Santella JB 3rd, Gardner DS, Yao W, Shi C, Reddy P, Tebben AJ, DeLucca GV, Wacker DA, Watson PS, Welch PK, Wadman EA, Davies P, Solomon KA, Graden DM, Yeleswaram S, Mandlekar S, Kariv I, Decicco CP, Ko SS, Carter PH, Duncia JV. Santella JB 3rd, et al. Among authors: kariv i. Bioorg Med Chem Lett. 2008 Jan 15;18(2):576-85. doi: 10.1016/j.bmcl.2007.11.067. Epub 2007 Nov 22. Bioorg Med Chem Lett. 2008. PMID: 18096386
CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.
Pruitt JR, Batt DG, Wacker DA, Bostrom LL, Booker SK, McLaughlin E, Houghton GC, Varnes JG, Christ DD, Covington M, Das AM, Davies P, Graden D, Kariv I, Orlovsky Y, Stowell NC, Vaddi KG, Wadman EA, Welch PK, Yeleswaram S, Solomon KA, Newton RC, Decicco CP, Carter PH, Ko SS. Pruitt JR, et al. Among authors: kariv i. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2992-7. doi: 10.1016/j.bmcl.2007.03.065. Epub 2007 Mar 24. Bioorg Med Chem Lett. 2007. PMID: 17418570
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.
Rivkin A, Kim YR, Goulet MT, Bays N, Hill AD, Kariv I, Krauss S, Ginanni N, Strack PR, Kohl NE, Chung CC, Varnerin JP, Goudreau PN, Chang A, Tota MR, Munoz B. Rivkin A, et al. Among authors: kariv i. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4620-3. doi: 10.1016/j.bmcl.2006.06.014. Epub 2006 Jun 19. Bioorg Med Chem Lett. 2006. PMID: 16784844
Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors.
Close J, Heidebrecht R Jr, Hendrix J, Li C, Munoz B, Surdi L, Kattar S, Tempest P, Moses P, Geng X, Hughes B, Smotrov N, Moxham C, Chapnick J, Kariv I, Nikov G, Burke JE, Deshmukh S, Jeliazkova-Mecheva V, Leach JK, Diaz D, Xu L, Yang Z, Kwei G, Moy L, Shah S, Tanga F, Kenefic C, Savage D, Shearman M, Ball RG, McNevin MJ, Markarewicz A, Miller T. Close J, et al. Among authors: kariv i. Bioorg Med Chem Lett. 2012 May 1;22(9):3203-7. doi: 10.1016/j.bmcl.2012.03.038. Epub 2012 Mar 17. Bioorg Med Chem Lett. 2012. PMID: 22483609
Evaluation of JAK3 Biology in Autoimmune Disease Using a Highly Selective, Irreversible JAK3 Inhibitor.
Elwood F, Witter DJ, Piesvaux J, Kraybill B, Bays N, Alpert C, Goldenblatt P, Qu Y, Ivanovska I, Lee HH, Chiu CS, Tang H, Scott ME, Deshmukh SV, Zielstorff M, Byford A, Chakravarthy K, Dorosh L, Rivkin A, Klappenbach J, Pan BS, Kariv I, Dinsmore C, Slipetz D, Dandliker PJ. Elwood F, et al. Among authors: kariv i. J Pharmacol Exp Ther. 2017 May;361(2):229-244. doi: 10.1124/jpet.116.239723. Epub 2017 Feb 13. J Pharmacol Exp Ther. 2017. PMID: 28193636
MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H, Jewell JP, Kariv I, Katz JD, Kunii K, Lu W, Lutterbach BA, Paweletz CP, Qu X, Reilly JF, Szewczak AA, Zeng Q, Kohl NE, Dinsmore CJ. Pan BS, et al. Among authors: kariv i. Cancer Res. 2010 Feb 15;70(4):1524-33. doi: 10.1158/0008-5472.CAN-09-2541. Epub 2010 Feb 9. Cancer Res. 2010. PMID: 20145145
77 results