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Items: 1 to 20 of 102

1.

Pyridyl aminothiazoles as potent Chk1 inhibitors: optimization of cellular activity.

Dudkin VY, Wang C, Arrington KL, Fraley ME, Hartman GD, Stirdivant SM, Drakas RA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2613-9. doi: 10.1016/j.bmcl.2012.01.120.

PMID:
22365762
2.

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.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2609-12. doi: 10.1016/j.bmcl.2012.01.110.

PMID:
22374217
3.

Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.

Reader JC, Matthews TP, Klair S, Cheung KM, Scanlon J, Proisy N, Addison G, Ellard J, Piton N, Taylor S, Cherry M, Fisher M, Boxall K, Burns S, Walton MI, Westwood IM, Hayes A, Eve P, Valenti M, de Haven Brandon A, Box G, van Montfort RL, Williams DH, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I.

J Med Chem. 2011 Dec 22;54(24):8328-42. doi: 10.1021/jm2007326.

4.

Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.

Huang X, Cheng CC, Fischmann TO, Duca JS, Richards M, Tadikonda PK, Reddy PA, Zhao L, Siddiqui MA, Parry D, Davis N, Seghezzi W, Wiswell D, Shipps GW Jr.

Bioorg Med Chem Lett. 2013 May 1;23(9):2590-4. doi: 10.1016/j.bmcl.2013.02.108.

PMID:
23535330
5.

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.

PMID:
22551018
6.

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.

PMID:
17352464
7.

Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.

Teng M, Zhu J, Johnson MD, Chen P, Kornmann J, Chen E, Blasina A, Register J, Anderes K, Rogers C, Deng Y, Ninkovic S, Grant S, Hu Q, Lundgren K, Peng Z, Kania RS.

J Med Chem. 2007 Nov 1;50(22):5253-6.

PMID:
17887663
8.

Synthesis and biological activities of new checkpoint kinase 1 inhibitors structurally related to granulatimide.

Conchon E, Anizon F, Aboab B, Prudhomme M.

J Med Chem. 2007 Sep 20;50(19):4669-80.

PMID:
17722905
9.

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.

PMID:
22342147
10.

Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.

Misra RN, Xiao HY, Williams DK, Kim KS, Lu S, Keller KA, Mulheron JG, Batorsky R, Tokarski JS, Sack JS, Kimball SD, Lee FY, Webster KR.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2973-7.

PMID:
15125971
11.

Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.

Chen S, Chen L, Le NT, Zhao C, Sidduri A, Lou JP, Michoud C, Portland L, Jackson N, Liu JJ, Konzelmann F, Chi F, Tovar C, Xiang Q, Chen Y, Wen Y, Vassilev LT.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2134-8.

PMID:
17303421
12.

Identification of novel aminothiazole and aminothiadiazole conjugated cyanopyridines as selective CHK1 inhibitors.

Gomha SM, Abdulla MM, Abou-Seri SM.

Eur J Med Chem. 2015 Mar 6;92:459-70. doi: 10.1016/j.ejmech.2015.01.019.

PMID:
25594740
13.

Synthesis and evaluation of 5-substituted 9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as check point 1 kinase inhibitors.

Sako Y, Ichikawa S, Osada A, Matsuda A.

Bioorg Med Chem. 2010 Nov 15;18(22):7878-89. doi: 10.1016/j.bmc.2010.09.042.

PMID:
20943405
14.

Checkpoint kinase inhibitors: a patent review (2009 - 2010).

Lainchbury M, Collins I.

Expert Opin Ther Pat. 2011 Aug;21(8):1191-210. doi: 10.1517/13543776.2011.586632. Review.

PMID:
21599421
15.

Re-purposing clinical kinase inhibitors to enhance chemosensitivity by overriding checkpoints.

Beeharry N, Banina E, Hittle J, Skobeleva N, Khazak V, Deacon S, Andrake M, Egleston BL, Peterson JR, Astsaturov I, Yen TJ.

Cell Cycle. 2014;13(14):2172-91. doi: 10.4161/cc.29214.

16.

Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors.

McIntyre NA, McInnes C, Griffiths G, Barnett AL, Kontopidis G, Slawin AM, Jackson W, Thomas M, Zheleva DI, Wang S, Blake DG, Westwood NJ, Fischer PM.

J Med Chem. 2010 Mar 11;53(5):2136-45. doi: 10.1021/jm901660c.

PMID:
20146435
17.

A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway.

Huart AS, Saxty B, Merritt A, Nekulova M, Lewis S, Huang Y, Vojtesek B, Kettleborough C, Hupp TR.

Bioorg Med Chem Lett. 2013 Oct 15;23(20):5578-85. doi: 10.1016/j.bmcl.2013.08.046.

PMID:
24007918
18.

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Wang L, Sullivan GM, Hexamer LA, Hasvold LA, Thalji R, Przytulinska M, Tao ZF, Li G, Chen Z, Xiao Z, Gu WZ, Xue J, Bui MH, Merta P, Kovar P, Bouska JJ, Zhang H, Park C, Stewart KD, Sham HL, Sowin TJ, Rosenberg SH, Lin NH.

J Med Chem. 2007 Aug 23;50(17):4162-76.

PMID:
17658776
19.

Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors.

Le Brazidec JY, Pasis A, Tam B, Boykin C, Wang D, Marcotte DJ, Claassen G, Chong JH, Chao J, Fan J, Nguyen K, Silvian L, Ling L, Zhang L, Choi M, Teng M, Pathan N, Zhao S, Li T, Taveras A.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4033-7. doi: 10.1016/j.bmcl.2012.04.085.

PMID:
22607669
20.

Docking-based 3D-QSAR study of pyridyl aminothiazole derivatives as checkpoint kinase 1 inhibitors.

Balupuri A, Balasubramanian PK, Gadhe CG, Cho SJ.

SAR QSAR Environ Res. 2014;25(8):651-71. doi: 10.1080/1062936X.2014.923040.

PMID:
24911214
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