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Publikationer i urvalet

27 träffar

Bibliografisk träff 2024-03-18

Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation.

Dou X, Huo T, Liu Y, Pang Z, Su L, Zhao X, Peng X, Liu Z, Zhang L, Jiao N.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2024.116323

Bibliografisk träff 2023-12-20

Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors.

Takarada JE, Cunha MR, Almeida VM, Vasconcelos SNS, Santiago AS, Godoi PH, Salmazo A, Ramos PZ, Fala AM, de Souza LR, Da Silva IEP, Bengtson MH, Massirer KB, Couñago RM.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2023.117561

Bibliografisk träff 2021-03-10

Synergistic effects of type I PRMT and PARP inhibitors against non-small cell lung cancer cells.

Dominici C, Sgarioto N, Yu Z, Sesma-Sanz L, Masson JY, Richard S, Raynal NJ.

Clin Epigenetics · research support, non-u.s. gov't; research-article; journal article · DOI 10.1186/s13148-021-01037-1

Bibliografisk träff 2020-01-31

Design, synthesis, biological evaluation of 6-(2-amino-1H-benzo[d]imidazole-6-yl)quinazolin-4(3H)-one derivatives as novel anticancer agents with Aurora kinase inhibition.

Fan C, Zhong T, Yang H, Yang Y, Wang D, Yang X, Xu Y, Fan Y.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112108

Bibliografisk träff 2019-11-11

Generation of highly potent DYRK1A-dependent inducers of human β-Cell replication via Multi-Dimensional compound optimization.

Allegretti PA, Horton TM, Abdolazimi Y, Moeller HP, Yeh B, Caffet M, Michel G, Smith M, Annes JP.

Bioorg Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2019.115193

Bibliografisk träff 2018-11-07

Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors.

Sang CY, Qin WW, Zhang XJ, Xu Y, Ma YZ, Wang XR, Hui L, Chen SW.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2018.11.006

Bibliografisk träff 2018-06-01

Discovery and optimization of novel benzothiophene-3-carboxamides as highly potent inhibitors of Aurora kinases A and B.

Gyulavári P, Szokol B, Szabadkai I, Brauswetter D, Bánhegyi P, Varga A, Markó P, Boros S, Illyés E, Szántai-Kis C, Krekó M, Czudor Z, Őrfi L.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2018.05.064

Bibliografisk träff 2017-12-01

The target landscape of clinical kinase drugs.

Klaeger S, Heinzlmeir S, Wilhelm M, Polzer H, Vick B, Koenig PA, Reinecke M, Ruprecht B, Petzoldt S, Meng C, Zecha J, Reiter K, Qiao H, Helm D, Koch H, Schoof M, Canevari G, Casale E, Depaolini SR, Feuchtinger A, Wu Z, Schmidt T, Rueckert L, Becker W, Huenges J, Garz AK, Gohlke BO, Zolg DP, Kayser G, Vooder T, Preissner R, Hahne H, Tõnisson N, Kramer K, Götze K, Bassermann F, Schlegl J, Ehrlich HC, Aiche S, Walch A, Greif PA, Schneider S, Felder ER, Ruland J, Médard G, Jeremias I, Spiekermann K, Kuster B.

Science · research support, non-u.s. gov't; research-article; journal article · DOI 10.1126/science.aan4368

Bibliografisk träff 2017-08-24

A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies.

Borisa AC, Bhatt HG.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2017.08.045

Bibliografisk träff 2015-08-01

Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma.

Siegel MB, Liu SQ, Davare MA, Spurgeon SE, Loriaux MM, Druker BJ, Scott EC, Tyner JW.

Oncotarget · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.18632/oncotarget.4214

Bibliografisk träff 2015-04-22

MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.

Sells TB, Chau R, Ecsedy JA, Gershman RE, Hoar K, Huck J, Janowick DA, Kadambi VJ, LeRoy PJ, Stirling M, Stroud SG, Vos TJ, Weatherhead GS, Wysong DR, Zhang M, Balani SK, Bolen JB, Manfredi MG, Claiborne CF.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml500409n

Bibliografisk träff 2014-03-12

Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.

Luo Y, Deng YQ, Wang J, Long ZJ, Tu ZC, Peng W, Zhang JQ, Liu Q, Lu G.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2014.03.027

Bibliografisk träff 2013-08-30

Selectivity data: assessment, predictions, concordance, and implications.

Gao C, Cahya S, Nicolaou CA, Wang J, Watson IA, Cummins DJ, Iversen PW, Vieth M.

J Med Chem · journal article · DOI 10.1021/jm400798j

Bibliografisk träff 2012-08-30

Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.

Lawrence HR, Martin MP, Luo Y, Pireddu R, Yang H, Gevariya H, Ozcan S, Zhu JY, Kendig R, Rodriguez M, Elias R, Cheng JQ, Sebti SM, Schonbrunn E, Lawrence NJ.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm300334d

Bibliografisk träff 2012-01-18

Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1.

Le Brazidec JY, Pasis A, Tam B, Boykin C, Black C, Wang D, 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 · journal article · DOI 10.1016/j.bmcl.2012.01.019

Bibliografisk träff 2011-10-30

Comprehensive analysis of kinase inhibitor selectivity.

Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP.

Nat Biotechnol · journal article · DOI 10.1038/nbt.1990

Bibliografisk träff 2011-03-03

Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.

Shallal HM, Russu WA.

Eur J Med Chem · research support, non-u.s. gov't; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1016/j.ejmech.2011.02.057

Bibliografisk träff 2010-12-01

Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase.

Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J.

Cancer Res · journal article · DOI 10.1158/0008-5472.can-10-2101

Bibliografisk träff 2010-09-01

Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.

Cee VJ, Schenkel LB, Hodous BL, Deak HL, Nguyen HN, Olivieri PR, Romero K, Bak A, Be X, Bellon S, Bush TL, Cheng AC, Chung G, Coats S, Eden PM, Hanestad K, Gallant PL, Gu Y, Huang X, Kendall RL, Lin MH, Morrison MJ, Patel VF, Radinsky R, Rose PE, Ross S, Sun JR, Tang J, Zhao H, Payton M, Geuns-Meyer SD.

J Med Chem · journal article · DOI 10.1021/jm100394y

Bibliografisk träff 2010-08-21

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

Bouloc N, Large JM, Kosmopoulou M, Sun C, Faisal A, Matteucci M, Reynisson J, Brown N, Atrash B, Blagg J, McDonald E, Linardopoulos S, Bayliss R, Bavetsias V.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2010.08.091

Bibliografisk träff 2010-06-01

Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.

Wang S, Midgley CA, Scaërou F, Grabarek JB, Griffiths G, Jackson W, Kontopidis G, McClue SJ, McInnes C, Meades C, Mezna M, Plater A, Stuart I, Thomas MP, Wood G, Clarke RG, Blake DG, Zheleva DI, Lane DP, Jackson RC, Glover DM, Fischer PM.

J Med Chem · journal article · DOI 10.1021/jm901913s

Bibliografisk träff 2010-05-01

Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D.

J Med Chem · journal article · DOI 10.1021/jm901870q

Bibliografisk träff 2009-05-01

Discovery and development of aurora kinase inhibitors as anticancer agents.

Pollard JR, Mortimore M.

J Med Chem · review; journal article · DOI 10.1021/jm8012129

Bibliografisk träff 2009-05-01

A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.

Aliagas-Martin I, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Huang OW, Hunsaker T, Kleinheinz T, Krueger E, Liang J, Moffat J, Phillips G, Pulk R, Rawson TE, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhu BY, Cochran AG.

J Med Chem · research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/jm9000314

Bibliografisk träff 2008-01-01

A quantitative analysis of kinase inhibitor selectivity.

Karaman MW, Herrgard S, Treiber DK, Gallant P, Atteridge CE, Campbell BT, Chan KW, Ciceri P, Davis MI, Edeen PT, Faraoni R, Floyd M, Hunt JP, Lockhart DJ, Milanov ZV, Morrison MJ, Pallares G, Patel HK, Pritchard S, Wodicka LM, Zarrinkar PP.

Nat Biotechnol · journal article · DOI 10.1038/nbt1358

Bibliografisk träff 2007-02-23

Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.

Manfredi MG, Ecsedy JA, Meetze KA, Balani SK, Burenkova O, Chen W, Galvin KM, Hoar KM, Huck JJ, LeRoy PJ, Ray ET, Sells TB, Stringer B, Stroud SG, Vos TJ, Weatherhead GS, Wysong DR, Zhang M, Bolen JB, Claiborne CF.

Proc Natl Acad Sci U S A · research-article; journal article · DOI 10.1073/pnas.0608798104

Bibliografisk träff 2006-09-01

Aurora kinase inhibitors: a new class of targeted drugs in cancer.

Gautschi O, Mack PC, Davies AM, Lara PN, Gandara DR.

Clin Lung Cancer · research support, non-u.s. gov't; review; journal article · DOI 10.3816/clc.2006.n.036