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Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K(ATP) opener that selectively inhibits spontaneous bladder contractions.
Carroll WA, Altenbach RJ, Bai H, Brioni JD, Brune ME, Buckner SA, Cassidy C, Chen Y, Coghlan MJ, Daza AV, Drizin I, Fey TA, Fitzgerald M, Gopalakrishnan M, Gregg RJ, Henry RF, Holladay MW, King LL, Kort ME, Kym PR, Milicic I, Tang R, Turner SC, Whiteaker KL, Yi L, Zhang H, Sullivan JP. Carroll WA, et al. J Med Chem. 2004 Jun 3;47(12):3163-79. doi: 10.1021/jm030356w. J Med Chem. 2004. PMID: 15163196
Synthesis and structure-activity relationships of a novel series of tricyclic dihydropyridine-based KATP openers that potently inhibit bladder contractions in vitro.
Carroll WA, Agrios KA, Altenbach RJ, Buckner SA, Chen Y, Coghlan MJ, Daza AV, Drizin I, Gopalakrishnan M, Henry RF, Kort ME, Kym PR, Milicic I, Smith JC, Tang R, Turner SC, Whiteaker KL, Zhang H, Sullivan JP. Carroll WA, et al. J Med Chem. 2004 Jun 3;47(12):3180-92. doi: 10.1021/jm030357o. J Med Chem. 2004. PMID: 15163197
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.
Dinges J, Akritopoulou-Zanze I, Arnold LD, Barlozzari T, Bousquet PF, Cunha GA, Ericsson AM, Iwasaki N, Michaelides MR, Ogawa N, Phelan KM, Rafferty P, Sowin TJ, Stewart KD, Tokuyama R, Xia Z, Zhang HQ. Dinges J, et al. Among authors: zhang hq. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4371-5. doi: 10.1016/j.bmcl.2006.05.052. Epub 2006 Jun 5. Bioorg Med Chem Lett. 2006. PMID: 16750628
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: zhang hq. J Med Chem. 2007 May 3;50(9):2011-29. doi: 10.1021/jm061223o. Epub 2007 Apr 11. J Med Chem. 2007. PMID: 17425296
1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.
Dinges J, Ashworth KL, Akritopoulou-Zanze I, Arnold LD, Baumeister SA, Bousquet PF, Cunha GA, Davidsen SK, Djuric SW, Gracias VJ, Michaelides MR, Rafferty P, Sowin TJ, Stewart KD, Xia Z, Zhang HQ. Dinges J, et al. Among authors: zhang hq. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4266-71. doi: 10.1016/j.bmcl.2006.05.066. Epub 2006 Jun 12. Bioorg Med Chem Lett. 2006. PMID: 16759855
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