Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 4, 2006, Pages 1040-1044

  Cockcroft, Xiao Ling ^a   Dillon, Krystyna J ^a   Dixon, Lesley ^b   Drzewiecki, Jan ^a   Kerrigan, Frank ^b   Loh Jr , Vincent M ^a   Martin, Niall M B ^a   Menear, Keith A ^a   Smith, Graeme C M ^a  

^a KuDOS Pharmaceuticals Ltd   (United Kingdom)

^b NONE   (United Kingdom)

Author keywords

Anti cancer; BRCA2 deficient cell; DNA repair; PARP 1 inhibitor; Phthalazinone

Indexed keywords

4 4 BENZYL 2H PHTHALAZIN 1 ONE; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE INHIBITOR; PHTHALAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CRYSTAL STRUCTURE; DRUG EFFECT; DRUG INHIBITION; DRUG MECHANISM; DRUG SYNTHESIS; IC 50; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PHTHALAZINES; POLY(ADP-RIBOSE) POLYMERASES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 30344439130     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.10.081     Document Type: Article

References (12)

1. M. Satoh, and T. Lindahl Nature 356 1992 356
2. S. Szabo, B. Zingarelli, M. O'Connor, and A.L. Salzman J. Clin. Invest. 100 1997 723
3. O. Cantoni, F. Cattbeni, V. Stocchi, R.E. Meyn, P. Cerrutti, and D. Murray Biochem. Biophys. Acta 1014 1989 1
4. N.J. Curtin Expert Rev. Mol. Med. 7 2005 1
5. H.E. Bryant, N. Schultz, H.D. Thomas, K.M. Parker, D. Flower, E. Lopez, S. Kyle, M. Meouth, N.J. Curtin, and T. Helleday Nature 434 2005 913
6. H. Farmer, N. McCabe, C.J. Lord, A.N.J. Tutt, D.A. Johnson, T.B. Richardson, M. Santarosa, K.J. Dillon, I. Hickson, C. Knights, N.M.B. Martin, S.P. Jackson, G.C.M. Smith, and A. Ashworth Nature 434 2005 917
7. V.M. Loh, X. Cockcroft, K.J. Dillon, L. Dixon, J. Drzewiecki, P.J. Eversley, S. Gomez, J. Hoare, F. Kerrigan, I.T.W. Matthews, K.A. Menear, N.M.B. Martin, R.F. Newton, J. Paul, G.C.M. Smith, J. Vile, and A.J. Whittle Bioorg. Med. Chem. Lett. 15 2005 2235
8. K.J. Dillon, G.S. Smith, and N.M.B. Martin J. Biomol. Screen. 8 2003 347
9. A. Ruf, J.M. de Murcia, G. de Murcia, and G.E. Schulz Proc. Natl. Acad. Sci. U.S.A. 93 1996 7481
10. A. Ruf, G. de Murcia, and G.E. Schulz Biochemistry 37 1998 3893
11. MacroModel version 7.1, Schrödinger Inc. 1999-2000.
12. A.W. White, R. Almasy, H.A. Calvert, N.J. Curtin, R.J. Griffin, Z. Hostomsky, K. Maegley, D.R. Newell, and B.T. Golding J. Med. Chem. 43 2000 4084