ATTEMPTS TO INTRODUCE CHEMOTHERAPEUTIC NUCLEOTIDES INTO CELLS - STUDIES ON THE ANTI-HIV AGENT FDT

被引：19

作者：

MCGUIGAN, C

JONES, BCNM

DEVINE, KG

NICHOLLS, SR

OCONNOR, TJ

KINCHINGTON, D

机构：

[1] UNIV LONDON UNIV COLL,DEPT CHEM,LONDON WC1H 0AJ,ENGLAND

[2] ST BARTHOLOMEWS HOSP & MED COLL,DEPT VIROL,LONDON EC1A 7BE,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)81057-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Phosphate, phosphoramidate, and phosphorodiamidate derivatives of the anti-HIV nucleoside analogue FdT were prepared as potential pro-drugs of the bio-active free nucleotide. Two synthetic routes were adopted. The anti-viral activity of the derivatives varies greatly with the phosphate structure, but several are active below 1-mu-M.

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页码：729 / 732

页数：4

相关论文

共 20 条

[1] BIS(META-NITROPHENYL) AND BIS(PARA-NITROPHENYL) ESTERS AND THE PHOSPHORODIAMIDATE OF THYMIDINE 5'-PHOSPHATE AS POTENTIAL SOURCES OF INTRACELLULAR THYMIDINE 5'-PHOSPHATE IN MOUSE CELLS IN CULTURE [J].

CHAWLA, RR ;

FREED, JJ ;

HAMPTON, A .

JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (12) :1733-1736

[2] SOME STUDIES OF ACTIVE INTERMEDIATES FORMED IN MICROSOMAL METABOLISM OF CYCLOPHOSPHAMIDE AND ISOPHOSPHAMIDE [J].

CONNORS, TA ;

COX, PJ ;

FARMER, PB ;

FOSTER, AB ;

JARMAN, M .

BIOCHEMICAL PHARMACOLOGY, 1974, 23 (01) :115-129

[3]

CURLEY D, 1990, ANTIVIR RES, V14, P345, DOI 10.1016/0166-3542(90)90053-A

[4] INHIBITION OF HERPES-SIMPLEX VIRUS-INDUCED DNA-POLYMERASE ACTIVITY AND VIRAL-DNA REPLICATION BY 9-(2-HYDROXYETHOXYMETHYL)GUANINE AND ITS TRIPHOSPHATE [J].

FURMAN, PA ;

STCLAIR, MH ;

FYFE, JA ;

RIDEOUT, JL ;

KELLER, PM ;

ELION, GB .

JOURNAL OF VIROLOGY, 1979, 32 (01) :72-77

[5] 3'-SUBSTITUTED 2',3'-DIDEOXYNUCLEOSIDE ANALOGS AS POTENTIAL ANTI-HIV (HTLV-III/LAV) AGENTS [J].

HERDEWIJN, P ;

BALZARINI, J ;

DECLERCQ, E ;

PAUWELS, R ;

BABA, M ;

BRODER, S ;

VANDERHAEGHE, H .

JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (08) :1270-1278

[6] SYNTHESIS OF 2'-DEOXY-5-FLUORO-5'-O-1',3',2'-OXAZAPHOSPHACYCLOHEXA-2'-YLURIDINE 2'-OXIDE AND RELATED-COMPOUNDS [J].

HUNSTON, RN ;

JEHANGIR, M ;

JONES, AS ;

WALKER, RT .

TETRAHEDRON, 1980, 36 (16) :2337-2340

[7] SYNTHESIS OF SOME NUCLEOSIDE CYCLIC PHOSPHORAMIDATES AND RELATED-COMPOUNDS VIA PHOSPHORAMIDITES [J].

JONES, AS ;

MCGUIGAN, C ;

WALKER, RT .

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1985, (02) :199-202

[8]

JONES B C N M, 1991, Antiviral Chemistry and Chemotherapy, V2, P35

[9]

JONES BCN, 1989, NUCLEIC ACIDS RES, V17, P7195

[10] COMPARISON OF ANTIGEN CAPTURE ASSAYS AGAINST HIV-1 IN EVALUATING ANTIVIRAL COMPOUNDS [J].

KINCHINGTON, D ;

GALPIN, SA ;

OCONNOR, TJ ;

JEFFRIES, DJ ;

WILLIAMSON, JD .

AIDS, 1989, 3 (02) :101-104