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Items: 1 to 20 of 93

1.

Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.

Dowling JE, Alimzhanov M, Bao L, Block MH, Chuaqui C, Cooke EL, Denz CR, Hird A, Huang S, Larsen NA, Peng B, Pontz TW, Rivard-Costa C, Saeh JC, Thakur K, Ye Q, Zhang T, Lyne PD.

ACS Med Chem Lett. 2013 Jul 3;4(8):800-5. doi: 10.1021/ml400197u. eCollection 2013 Aug 8.

2.

Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.

Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D, Pollard H, Lee JW, Peng B, Thakur K, Ye Q, Zhang T, Brassil P, Racicot V, Bao L, Denz CR, Cooke E.

ACS Med Chem Lett. 2012 Jan 24;3(4):278-83. doi: 10.1021/ml200257n. eCollection 2012 Apr 12.

3.

Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.

Dowling JE, Alimzhanov M, Bao L, Chuaqui C, Denz CR, Jenkins E, Larsen NA, Lyne PD, Pontz T, Ye Q, Holdgate GA, Snow L, O'Connell N, Ferguson AD.

ACS Med Chem Lett. 2016 Jan 20;7(3):300-5. doi: 10.1021/acsmedchemlett.5b00452. eCollection 2016 Mar 10.

4.

Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.

Nie Z, Perretta C, Erickson P, Margosiak S, Almassy R, Lu J, Averill A, Yager KM, Chu S.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4191-5. Epub 2007 May 18.

PMID:
17540560
5.

Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities.

Nie Z, Perretta C, Erickson P, Margosiak S, Lu J, Averill A, Almassy R, Chu S.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):619-23. Epub 2007 Nov 28.

PMID:
18055206
6.

CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy.

Siddiqui-Jain A, Drygin D, Streiner N, Chua P, Pierre F, O'Brien SE, Bliesath J, Omori M, Huser N, Ho C, Proffitt C, Schwaebe MK, Ryckman DM, Rice WG, Anderes K.

Cancer Res. 2010 Dec 15;70(24):10288-98. doi: 10.1158/0008-5472.CAN-10-1893.

7.

Discovery of novel 2-anilinopyrazolo[1,5-a]pyrimidine derivatives as c-Src kinase inhibitors for the treatment of acute ischemic stroke.

Mukaiyama H, Nishimura T, Shiohara H, Kobayashi S, Komatsu Y, Kikuchi S, Tsuji E, Kamada N, Ohnota H, Kusama H.

Chem Pharm Bull (Tokyo). 2007 Jun;55(6):881-9.

8.

Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors.

Xu Y, Brenning BG, Kultgen SG, Foulks JM, Clifford A, Lai S, Chan A, Merx S, McCullar MV, Kanner SB, Ho KK.

ACS Med Chem Lett. 2014 Oct 22;6(1):63-7. doi: 10.1021/ml500300c. eCollection 2015 Jan 8.

9.

Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.

Yang LL, Li GB, Ma S, Zou C, Zhou S, Sun QZ, Cheng C, Chen X, Wang LJ, Feng S, Li LL, Yang SY.

J Med Chem. 2013 Feb 28;56(4):1641-55. doi: 10.1021/jm301537p. Epub 2013 Feb 19.

PMID:
23362959
10.

Diversity-oriented synthesis of pyrazolo[4,3-b]indoles by gold-catalysed three-component annulation: application to the development of a new class of CK2 inhibitors.

Hou Z, Oishi S, Suzuki Y, Kure T, Nakanishi I, Hirasawa A, Tsujimoto G, Ohno H, Fujii N.

Org Biomol Chem. 2013 May 28;11(20):3288-96. doi: 10.1039/c3ob40223a.

PMID:
23535832
11.

Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds.

Hou Z, Nakanishi I, Kinoshita T, Takei Y, Yasue M, Misu R, Suzuki Y, Nakamura S, Kure T, Ohno H, Murata K, Kitaura K, Hirasawa A, Tsujimoto G, Oishi S, Fujii N.

J Med Chem. 2012 Mar 22;55(6):2899-903. doi: 10.1021/jm2015167. Epub 2012 Mar 7.

PMID:
22339433
12.

Structure-based design of small peptide inhibitors of protein kinase CK2 subunit interaction.

Laudet B, Barette C, Dulery V, Renaudet O, Dumy P, Metz A, Prudent R, Deshiere A, Dideberg O, Filhol O, Cochet C.

Biochem J. 2007 Dec 15;408(3):363-73.

13.

Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.

Baraldi PG, Fruttarolo F, Tabrizi MA, Preti D, Romagnoli R, El-Kashef H, Moorman A, Varani K, Gessi S, Merighi S, Borea PA.

J Med Chem. 2003 Mar 27;46(7):1229-41.

PMID:
12646033
14.

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

Staben ST, Heffron TP, Sutherlin DP, Bhat SR, Castanedo GM, Chuckowree IS, Dotson J, Folkes AJ, Friedman LS, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Olivero AG, Plise E, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Tsui V, Wan NC, Wang S, Weismann C, Wu P, Zhu BY.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6048-51. doi: 10.1016/j.bmcl.2010.08.067. Epub 2010 Aug 19.

PMID:
20822905
15.

Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2.

Guillon J, Le Borgne M, Rimbault C, Moreau S, Savrimoutou S, Pinaud N, Baratin S, Marchivie M, Roche S, Bollacke A, Pecci A, Alvarez L, Desplat V, Jose J.

Eur J Med Chem. 2013 Jul;65:205-22. doi: 10.1016/j.ejmech.2013.04.051. Epub 2013 May 3.

PMID:
23711832
16.

Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system.

Azam MA, Dharanya L, Mehta CC, Sachdeva S.

Acta Pharm. 2013 Mar;63(1):19-30. doi: 10.2478/acph-2013-0001.

PMID:
23482310
17.

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2.

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

Bioorg Med Chem Lett. 2011 Jan 1;21(1):471-4. doi: 10.1016/j.bmcl.2010.10.114. Epub 2010 Oct 28.

PMID:
21094607
18.

Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.

Lim J, Altman MD, Baker J, Brubaker JD, Chen H, Chen Y, Fischmann T, Gibeau C, Kleinschek MA, Leccese E, Lesburg C, Maclean JK, Moy LY, Mulrooney EF, Presland J, Rakhilina L, Smith GF, Steinhuebel D, Yang R.

ACS Med Chem Lett. 2015 Apr 20;6(6):683-8. doi: 10.1021/acsmedchemlett.5b00107. eCollection 2015 Jun 11.

19.

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
20.

Protein kinase CK2 protects multiple myeloma cells from ER stress-induced apoptosis and from the cytotoxic effect of HSP90 inhibition through regulation of the unfolded protein response.

Manni S, Brancalion A, Tubi LQ, Colpo A, Pavan L, Cabrelle A, Ave E, Zaffino F, Di Maira G, Ruzzene M, Adami F, Zambello R, Pitari MR, Tassone P, Pinna LA, Gurrieri C, Semenzato G, Piazza F.

Clin Cancer Res. 2012 Apr 1;18(7):1888-900. doi: 10.1158/1078-0432.CCR-11-1789. Epub 2012 Feb 20.

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