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

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 12, 2012, Pages 4033-4037

  Le Brazidec, Jean Yves ^a   Pasis, Angela ^a   Tam, Betty ^a   Boykin, Christina ^a   Wang, Deping ^a   Marcotte, Douglas J ^a   Claassen, Gisela ^a   Chong, Jer Hong ^a   Chao, Jianhua ^a   Fan, Junhua ^a   Nguyen, Khanh ^a   Silvian, Laura ^a   Ling, Leona ^a   Zhang, Lin ^a   Choi, Michael ^a   Teng, Min ^a   Pathan, Nuzhat ^a   Zhao, Shuo ^a   Li, Tony ^a   Taveras, Art ^a  

^a BIOGEN   (United States)

Author keywords

Aurora kinase; Cell cycle arrest; Cyclin dependent kinase; Cytotoxicity; Pyrrolopyrimidine

Indexed keywords

AURORA KINASE INHIBITOR; PYRIMIDINE DERIVATIVE;

ARTICLE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; IN VITRO STUDY; STRUCTURE ACTIVITY RELATION;

ANTINEOPLASTIC AGENTS; BINDING SITES; CDC2 PROTEIN KINASE; CELL CYCLE CHECKPOINTS; CELL LINE; CYCLIN-DEPENDENT KINASE 2; DRUG DESIGN; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PYRIMIDINES; PYRROLES; STRUCTURAL HOMOLOGY, PROTEIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84861578184     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.04.085     Document Type: Article

References (9)

1. A.A. Dar, L.W. Goff, S. Majid, J. Berlin, and w. El-Rifai Mol. Cancer Ther. 9 2010 268
2. R. Bayliss, T. Sardon, I. Vernos, and E. Conti Mol. Cell 12 2003 851
3. S. Ulisse, E. Baldini, M. Toller, J.G. Delcros, A. Guého, F. Curcio, E. De Antoni, L. Giacomelli, F.S. Ambesi-Impiombato, S. Bocchini, M. D'Armiento, and Y. Arlot-Bonnemains Endocr. Relat. Cancer 14 2007 827
4. F. Sessa, M. Mapelli, C. Ciferri, C. Tarricone, L.B. Areces, T.R. Schneider, P.D. Stukenberg, and A. Musacchio Mol. Cell 18 2005 379
5. J.-Y. Le Brazidec, A. Pasis, B. Tam, C. Boykin, C. Black, D. Wang, G. Claassen, J.-H. Chong, J. Chao, J. Fan, K. Nguyen, L. Silvian, L. Ling, L. Zhang, M. Choi, M. Teng, N. Pathan, S. Zhao, T. Li, and A. Taveras Bioorg. Med. Chem. Lett. 22 2012 2070
6. M. Malumbres, and M. Barbacid Nat. Rev. Cancer 9 2009 153
7. G.M.T. Cheetham, R.M.A. Knegtel, J.T. Coll, S.B. Renwick, L. Swenson, P. Weber, J.A. Lippke, and D.A. Austen J. Biol. Chem. 277 45 2002 42419
8. X. Xiong, and M.C. Pirrung Org. Lett. 10 2008 1151
9. Molecular Operating Environment (MOE), 2010.10; Chemical Computing Group Inc., 1010 Sherbooke St. West, Suite #910, Montreal, QC, Canada, H3A 2R7, 2010.