ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
X-ray crystallography and computer-assisted molecular modeling (CAMM) studies aided in the design of a potent series of mammalian purine nucleoside phosphorylase (PNP) inhibitors. Enhanced potency was achieved by designing substituted 9-(arylmethyl)-9-deazaguanine analogs that interact favorably with all three of the binding subsites of the PNP active site, namely the purine binding site, the hydrophobic pocket, and the phosphate binding site. The most potent PNP inhibitor prepared during our investigation, (S)-9-[1-(3-chlorophenyl)-2-carboxyethyl]-9-deazaguanine (18b), was shown to have an IC50 of 6 nM, whereas the corresponding (R)-isomer was 30-fold less potent.
Wayne C. Guida合作论文数Department of Chemistry, University of South Florida;H. Lee Moffitt Cancer Center & Research Institute, University of South Florida3
Mark D. Erion合作论文数Merck & Co., Inc.3
Shri Niwas合作论文数2John A. Montgomery合作论文数2Y. S. BABU合作论文数2Charles E. Bugg合作论文数2
Steven Edward Ealick合作论文数Department of Chemistry and Chemical Biology, College of Arts & Sciences, Cornell University2Jerry D. Rose合作论文数2
Subramaniam Ananthan合作论文数Division of Neuroscience and Behavior, National Institute on Drug Abuse;National Institutes of Health2S Ananthan合作论文数1J D Rose合作论文数1Ja Secrist合作论文数1Ce Bugg合作论文数1S Niwas合作论文数1John A. Secrist合作论文数1Y. Sudhakar Babu合作论文数1
