SYNTHESIS OF PEPTIDE ANALOGS CONTAINING PHOSPHONAMIDATE METHYL-ESTER FUNCTIONALITY - HIV-1 PROTEINASE-INHIBITORS POSSESSING UNIQUE CELL UPTAKE PROPERTIES

被引：21

作者：

CAMP, NP

PERREY, DA

KINCHINGTON, D

HAWKINS, PCD

GANI, D

机构：

[1] UNIV ST ANDREWS, SCH CHEM, ST ANDREWS KY16 9ST, FIFE, Scotland

[2] ST BARTHOLOMEWS HOSP, DEPT VIROL, LONDON EC1A 7BE, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1995年 / 3卷 / 03期

关键词：

D O I：

10.1016/0968-0896(95)00022-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Stereochemically defined and epimeric phosphonamidate methyl ester-containing peptide analogues were synthesised and were found to be moderate inhibitors of the HIV-1 proteinase. All of the analogues containing the phosphonamidate ester grouping showed a marked ability to enter cells, as highlighted by the approximate equivalence of the IC50 values for enzyme inhibition in solution and inhibition of HIV-1 replication in virus infected cells.

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页码：297 / 312

页数：16

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