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Items: 1 to 20 of 108

1.

Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.

Oza V, Ashwell S, Brassil P, Breed J, Deng C, Ezhuthachan J, Haye H, Horn C, Janetka J, Lyne P, Newcombe N, Otterbien L, Pass M, Read J, Roswell S, Su M, Toader D, Yu D, Yu Y, Valentine A, Webborn P, White A, Zabludoff S, Zheng X.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5133-8. doi: 10.1016/j.bmcl.2010.07.015. Epub 2010 Jul 29.

PMID:
20673630
2.

Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.

Oza V, Ashwell S, Brassil P, Breed J, Ezhuthachan J, Deng C, Grondine M, Horn C, Liu D, Lyne P, Newcombe N, Pass M, Read J, Su M, Toader D, Yu D, Yu Y, Zabludoff S.

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2330-7. doi: 10.1016/j.bmcl.2012.01.043. Epub 2012 Feb 1.

PMID:
22342147
3.

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.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5989-94. Epub 2007 Aug 19.

PMID:
17804227
4.

Identification of inhibitors of checkpoint kinase 1 through template screening.

Matthews TP, Klair S, Burns S, Boxall K, Cherry M, Fisher M, Westwood IM, Walton MI, McHardy T, Cheung KM, Van Montfort R, Williams D, Aherne GW, Garrett MD, Reader J, Collins I.

J Med Chem. 2009 Aug 13;52(15):4810-9. doi: 10.1021/jm900314j.

PMID:
19572549
5.

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.

Janetka JW, Almeida L, Ashwell S, Brassil PJ, Daly K, Deng C, Gero T, Glynn RE, Horn CL, Ioannidis S, Lyne P, Newcombe NJ, Oza VB, Pass M, Springer SK, Su M, Toader D, Vasbinder MM, Yu D, Yu Y, Zabludoff SD.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4242-8. doi: 10.1016/j.bmcl.2008.05.016. Epub 2008 May 6.

PMID:
18547806
6.

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.

Dwyer MP, Paruch K, Labroli M, Alvarez C, Keertikar KM, Poker C, Rossman R, Fischmann TO, Duca JS, Madison V, Parry D, Davis N, Seghezzi W, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):467-70. doi: 10.1016/j.bmcl.2010.10.113. Epub 2010 Oct 27.

PMID:
21094608
7.

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.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1240-4. doi: 10.1016/j.bmcl.2008.12.076. Epub 2008 Dec 24.

PMID:
19155174
8.

Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.

Gazzard L, Appleton B, Chapman K, Chen H, Clark K, Drobnick J, Goodacre S, Halladay J, Lyssikatos J, Schmidt S, Sideris S, Wiesmann C, Williams K, Wu P, Yen I, Malek S.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5704-5709. doi: 10.1016/j.bmcl.2014.10.063. Epub 2014 Oct 27.

PMID:
25453805
9.

Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.

Oza V, Ashwell S, Almeida L, Brassil P, Breed J, Deng C, Gero T, Grondine M, Horn C, Ioannidis S, Liu D, Lyne P, Newcombe N, Pass M, Read J, Ready S, Rowsell S, Su M, Toader D, Vasbinder M, Yu D, Yu Y, Xue Y, Zabludoff S, Janetka J.

J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4.

PMID:
22551018
10.

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.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6049-53. Epub 2006 Sep 15.

PMID:
16978863
11.

Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.

Palmer WS, Alam M, Arzeno HB, Chang KC, Dunn JP, Goldstein DM, Gong L, Goyal B, Hermann JC, Hogg JH, Hsieh G, Jahangir A, Janson C, Jin S, Ursula Kammlott R, Kuglstatter A, Lukacs C, Michoud C, Niu L, Reuter DC, Shao A, Silva T, Trejo-Martin TA, Stein K, Tan YC, Tivitmahaisoon P, Tran P, Wagner P, Weller P, Wu SY.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1486-92. doi: 10.1016/j.bmcl.2012.12.047. Epub 2012 Dec 22.

PMID:
23352510
12.

Checkpoint kinase inhibitors: a review of the patent literature.

Janetka JW, Ashwell S.

Expert Opin Ther Pat. 2009 Feb;19(2):165-97. doi: 10.1517/13543770802653622. Review.

PMID:
19441917
13.

Context-dependent cell cycle checkpoint abrogation by a novel kinase inhibitor.

Massey AJ, Borgognoni J, Bentley C, Foloppe N, Fiumana A, Walmsley L.

PLoS One. 2010 Oct 18;5(10):e13123. doi: 10.1371/journal.pone.0013123.

14.

Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.

Tao ZF, Wang L, Stewart KD, Chen Z, Gu W, Bui MH, Merta P, Zhang H, Kovar P, Johnson E, Park C, Judge R, Rosenberg S, Sowin T, Lin NH.

J Med Chem. 2007 Apr 5;50(7):1514-27. Epub 2007 Mar 13.

PMID:
17352464
15.

Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.

Lin NH, Xia P, Kovar P, Park C, Chen Z, Zhang H, Rosenberg SH, Sham HL.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):421-6. Epub 2005 Oct 18.

PMID:
16242328
16.

Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.

Tao ZF, Li G, Tong Y, Stewart KD, Chen Z, Bui MH, Merta P, Park C, Kovar P, Zhang H, Sham HL, Rosenberg SH, Sowin TJ, Lin NH.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5944-51. Epub 2007 Aug 25.

PMID:
17827013
17.

Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.

Tong Y, Claiborne A, Stewart KD, Park C, Kovar P, Chen Z, Credo RB, Gu WZ, Gwaltney SL 2nd, Judge RA, Zhang H, Rosenberg SH, Sham HL, Sowin TJ, Lin NH.

Bioorg Med Chem. 2007 Apr 1;15(7):2759-67. Epub 2007 Jan 17.

PMID:
17287122
18.

Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.

Garbaccio RM, Huang S, Tasber ES, Fraley ME, Yan Y, Munshi S, Ikuta M, Kuo L, Kreatsoulas C, Stirdivant S, Drakas B, Rickert K, Walsh ES, Hamilton KA, Buser CA, Hardwick J, Mao X, Beck SC, Abrams MT, Tao W, Lobell R, Sepp-Lorenzino L, Hartman GD.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6280-5. Epub 2007 Sep 7.

PMID:
17900896
19.

Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.

Nishiguchi GA, Atallah G, Bellamacina C, Burger MT, Ding Y, Feucht PH, Garcia PD, Han W, Klivansky L, Lindvall M.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6366-9. doi: 10.1016/j.bmcl.2011.08.105. Epub 2011 Sep 10.

PMID:
21945284
20.

O-linked triazolotriazines: potent and selective c-Met inhibitors.

Chen F, Wang Y, Ai J, Zhan Z, Lv Y, Liang Z, Luo C, Mei D, Geng M, Duan W.

ChemMedChem. 2012 Jul;7(7):1276-85. doi: 10.1002/cmdc.201200145. Epub 2012 Apr 26.

PMID:
22539497

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