DESIGN AND SYNTHESIS OF NOVEL MONOCYCLIC BETA-LACTAM INHIBITORS OF PROSTATE-SPECIFIC ANTIGEN

Authors
ADLINGTON RM BALDWIN JE CHEN BN COOPER SL MCCOULL W PRITCHARD GJ HOWE TJ BECKER GW HERMANN RB MCNULTY AM NEUBAUER BL
Citation
Rm. Adlington et al., DESIGN AND SYNTHESIS OF NOVEL MONOCYCLIC BETA-LACTAM INHIBITORS OF PROSTATE-SPECIFIC ANTIGEN, Bioorganic & medicinal chemistry letters, 7(13), 1997, pp. 1689-1694
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
13
Year of publication
1997
Pages
1689 - 1694
Database
ISI
SICI code
0960-894X(1997)7:13<1689:DASONM>2.0.ZU;2-7
Abstract
A novel series of monocyclic B-lactam analogues was designed using a h omology derived model of prostate specific antigen (PSA) and by applic ation of a multiple copy simultaneous search technique. Syntheses were conducted by assembly of the B-lactam core via a Staudinger reaction with elaboration at the 1, 3 and 4 positions to probe active site bind ing. Inhibition against PSA was evaluated. (C) 1997 Elsevier Science L td.