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Page 1
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: kreatsoulas c. 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: kreatsoulas c. 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
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: kreatsoulas c. 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
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: kreatsoulas c. 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
Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates.
Dudkin VY, Rickert K, Kreatsoulas C, Wang C, Arrington KL, Fraley ME, Hartman GD, Yan Y, Ikuta M, Stirdivant SM, Drakas RA, Walsh ES, Hamilton K, Buser CA, Lobell RB, Sepp-Lorenzino L. Dudkin VY, et al. Among authors: kreatsoulas c. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2609-12. doi: 10.1016/j.bmcl.2012.01.110. Epub 2012 Feb 9. Bioorg Med Chem Lett. 2012. PMID: 22374217
Identification of potent, highly constrained CGRP receptor antagonists.
Stump CA, Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hershey JC, Jelley R, Kreatsoulas C, Moore EL, Mosser SD, Quigley AG, Roller SA, Salvatore CA, Sharik SS, Theberge CR, Zartman CB, Kane SA, Graham SL, Selnick HG, Vacca JP, Williams TM. Stump CA, et al. Among authors: kreatsoulas c. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2572-6. doi: 10.1016/j.bmcl.2010.02.086. Epub 2010 Feb 25. Bioorg Med Chem Lett. 2010. PMID: 20299218
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.
Ma L, Seager MA, Wittmann M, Jacobson M, Bickel D, Burno M, Jones K, Graufelds VK, Xu G, Pearson M, McCampbell A, Gaspar R, Shughrue P, Danziger A, Regan C, Flick R, Pascarella D, Garson S, Doran S, Kreatsoulas C, Veng L, Lindsley CW, Shipe W, Kuduk S, Sur C, Kinney G, Seabrook GR, Ray WJ. Ma L, et al. Among authors: kreatsoulas c. Proc Natl Acad Sci U S A. 2009 Sep 15;106(37):15950-5. doi: 10.1073/pnas.0900903106. Epub 2009 Aug 26. Proc Natl Acad Sci U S A. 2009. PMID: 19717450 Free PMC article.
Current and Future Roles of Artificial Intelligence in Medicinal Chemistry Synthesis.
Struble TJ, Alvarez JC, Brown SP, Chytil M, Cisar J, DesJarlais RL, Engkvist O, Frank SA, Greve DR, Griffin DJ, Hou X, Johannes JW, Kreatsoulas C, Lahue B, Mathea M, Mogk G, Nicolaou CA, Palmer AD, Price DJ, Robinson RI, Salentin S, Xing L, Jaakkola T, Green WH, Barzilay R, Coley CW, Jensen KF. Struble TJ, et al. Among authors: kreatsoulas c. J Med Chem. 2020 Aug 27;63(16):8667-8682. doi: 10.1021/acs.jmedchem.9b02120. Epub 2020 Apr 14. J Med Chem. 2020. PMID: 32243158 Free PMC article.
Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.
Haffner CD, Charnley AK, Aquino CJ, Casillas L, Convery MA, Cox JA, Elban MA, Goodwin NC, Gough PJ, Haile PA, Hughes TV, Knapp-Reed B, Kreatsoulas C, Lakdawala AS, Li H, Lian Y, Lipshutz D, Mehlmann JF, Ouellette M, Romano J, Shewchuk L, Shu A, Votta BJ, Zhou H, Bertin J, Marquis RW. Haffner CD, et al. Among authors: kreatsoulas c. ACS Med Chem Lett. 2019 Oct 11;10(11):1518-1523. doi: 10.1021/acsmedchemlett.9b00141. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749904 Free PMC article.
50 results