Design and synthesis of novel monocyclic beta-lactam inhibitors of prostate specific antigen

被引：81
作者：
Adlington, RM
Baldwin, JE
Chen, BN
Cooper, SL
McCoull, W
Pritchard, GJ
Howe, TJ
Becker, GW
Hermann, RB
McNulty, AM
Neubauer, BL
机构：
[1] UNIV OXFORD,DYSON PERRINS LAB,OXFORD OX1 3QY,ENGLAND
[2] LILLY RES CTR LTD,WINDLESHAM GU20 6PH,SURREY,ENGLAND
[3] LILLY CORP CTR,LILLY RES LABS,INDIANAPOLIS,IN 46285
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 13期
关键词：
D O I：
10.1016/S0960-894X(97)00285-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of monocyclic B-lactam analogues was designed using a homology derived model of prostate specific antigen (PSA) and by application 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 binding. Inhibition against PSA was evaluated. (C) 1997 Elsevier Science Ltd.
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页码：1689 / 1694
页数：6
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