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Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.
Akritopoulou-Zanze I, Wakefield BD, Gasiecki A, Kalvin D, Johnson EF, Kovar P, Djuric SW. Akritopoulou-Zanze I, et al. Among authors: gasiecki a. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1480-3. doi: 10.1016/j.bmcl.2011.01.001. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21288717
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.
Akritopoulou-Zanze I, Wakefield BD, Gasiecki A, Kalvin D, Johnson EF, Kovar P, Djuric SW. Akritopoulou-Zanze I, et al. Among authors: gasiecki a. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1476-9. doi: 10.1016/j.bmcl.2011.01.007. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21282054
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ. Dinges J, et al. Among authors: gasiecki af. J Med Chem. 2007 May 3;50(9):2011-29. doi: 10.1021/jm061223o. Epub 2007 Apr 11. J Med Chem. 2007. PMID: 17425296
Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase.
Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Liang CD, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG. Penning TD, et al. Among authors: gasiecki af. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3383-6. doi: 10.1016/s0960-894x(02)00760-6. Bioorg Med Chem Lett. 2002. PMID: 12419366
Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase.
Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Malecha JW, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG. Penning TD, et al. Among authors: gasiecki af. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1137-9. doi: 10.1016/s0960-894x(03)00039-8. Bioorg Med Chem Lett. 2003. PMID: 12643929
Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.
Penning TD, Chandrakumar NS, Chen BB, Chen HY, Desai BN, Djuric SW, Docter SH, Gasiecki AF, Haack RA, Miyashiro JM, Russell MA, Yu SS, Corley DG, Durley RC, Kilpatrick BF, Parnas BL, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Krivi GG, Villani-Price D, Pyla EY, Smith WG. Penning TD, et al. Among authors: gasiecki af. J Med Chem. 2000 Feb 24;43(4):721-35. doi: 10.1021/jm990496z. J Med Chem. 2000. PMID: 10691697
Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization.
Nagarajan SR, Lu HF, Gasiecki AF, Khanna IK, Parikh MD, Desai BN, Rogers TE, Clare M, Chen BB, Russell MA, Keene JL, Duffin T, Engleman VW, Finn MB, Freeman SK, Klover JA, Nickols GA, Nickols MA, Shannon KE, Steininger CA, Westlin WF, Westlin MM, Williams ML. Nagarajan SR, et al. Among authors: gasiecki af. Bioorg Med Chem. 2007 May 15;15(10):3390-412. doi: 10.1016/j.bmc.2007.03.020. Epub 2007 Mar 13. Bioorg Med Chem. 2007. PMID: 17387018
22 results