Novel, potent inhibitors of 17β-hydroxysteroid dehydrogenase type 1

Molecular and Cellular Endocrinology

Volumn 248, Issue 1-2, 2006, Pages 204-207

  Allan, Gillian M ^a   Bubert, Christian ^a   Vicker, Nigel ^a   Smith, Andrew ^a   Tutill, Helena J ^b   Purohit, Atul ^b   Reed, Michael J ^b   Potter, Barry V L ^a  

^a UNIVERSITY OF BATH   (United Kingdom)

^b ST MARY S HOSPITAL   (United Kingdom)

Author keywords

17 HSD1; Cancer; Estrone; Hydroxysteroid dehydrogenase; Inhibitor; Pyrazole

Indexed keywords

17BETA HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITOR; AMIDE; ENZYME INHIBITOR; PYRAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

CONFERENCE PAPER; CONTROLLED STUDY; DRUG ACTIVITY; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

AMIDES; ENZYME INHIBITORS; ESTRADIOL DEHYDROGENASES; ESTRONE; HUMANS; PYRAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR CELLS, CULTURED;

EID: 33644891865     PISSN: 03037207     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.mce.2005.10.021     Document Type: Conference Paper

References (7)

1. H.M. Berman, J. Westbrook, Z. Feng, G. Gilliland, T.N. Bhat, H. Weissig, I.N. Shindyalov, and P.E. Bourne The protein data bank Nucleic Acids Res. 28 2000 235 242
2. (+) identifies two principal targets for the design of inhibitors Structure 4 1996 905 915
3. L.J. Duncan, and M.J. Reed The role and proposed mechanism by which oestradiol 17 beta-hydroxysteroid dehydrogenase regulates breast tumour oestrogen concentrations J. Steroid Biochem. Mol. Biol. 55 1995 565 572
4. Ferlay, J., Bray, F., Pisani, P., Parkin, D. M., 2004. Globocan 2002: Cancer Incidence, Mortality and Prevalence Worldwide, Version 2.0. IARC Cancerbase No. 5. IARC Press, Lyon, France, 2004.
5. G. Jones, P. Willett, R.C. Glen, A.R. Leach, and R. Taylor Development and validation of a genetic algorithm for flexible docking J. Mol. Biol. 267 1997 727 748
6. H. Lawrence, N. Vicker, G.M. Allan, A. Smith, M. Mahon, H.J. Tutill, A. Purohit, M.J. Reed, and B.V.L. Potter Novel and potent 17β-hydroxysteroid dehydrogenase type 1 inhibitors J. Med. Chem. 48 2005 2759 2762
7. F. Sweet, J. Boyd, O. Medina, L. Konderski, and G.L. Murdock Hydrogen-bonding in steroidogenesis - studies on new heterocyclic-analogs of estrone that inhibit human estradiol 17-beta-dehydrogenase Biochem. Biophys. Res. Commun. 180 1991 1057 1063