PHOSPHATE DERIVATIVES OF D4T AS INHIBITORS OF HIV

被引:30
作者
MCGUIGAN, C
SHEEKA, HM
MAHMOOD, N
HAY, A
机构
[1] MRC,COLLABORAT CTR,LONDON NW7 1AD,ENGLAND
[2] NATL INST MED RES,LONDON NW7 1AA,ENGLAND
关键词
D O I
10.1016/S0960-894X(00)80315-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Phosphate derivatives of the anti-HIV nucleoside analogue d4T were prepared as potential pro-drugs of the bio-active free nucleotide. The anti-viral activity of the derivatives varies greatly with the phosphate structure. but several are active below 1 muM. All of the compounds are less toxic than the parent nucleoside analogue; in one case this leads to enhanced antiviral selectivity.
引用
收藏
页码:1203 / 1206
页数:4
相关论文
共 18 条
[1]  
BALZARINI J, 1989, J BIOL CHEM, V264, P6127
[2]   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
[3]  
HITCHCOCK M J M, 1991, Antiviral Chemistry and Chemotherapy, V2, P125
[4]   NUCLEOSIDES .9. FORMATION OF 2',3'-UNSATURATED PHYRIMIDINE NUCLEOSIDES VIA A NOVEL BETA-ELIMINATION REACTION [J].
HORWITZ, JP ;
CHUA, J ;
DAROOGE, MA ;
NOEL, M ;
KLUNDT, IL .
JOURNAL OF ORGANIC CHEMISTRY, 1966, 31 (01) :205-&
[5]  
JONES BCN, 1989, NUCLEIC ACIDS RES, V17, P7195
[6]   1-(2,3-DIDEOXY-BETA-D-GLYCERO-PENT-2-ENOFURANOSYL)THYMINE - A HIGHLY POTENT AND SELECTIVE ANTI-HIV AGENT [J].
MANSURI, MM ;
STARRETT, JE ;
GHAZZOULI, I ;
HITCHCOCK, MJM ;
STERZYCKI, RZ ;
BRANKOVAN, V ;
LIN, TS ;
AUGUST, EM ;
PRUSOFF, WH ;
SOMMADOSSI, JP ;
MARTIN, JC .
JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (02) :461-466
[7]   COMPARISON OF INVITRO BIOLOGICAL PROPERTIES AND MOUSE TOXICITIES OF 3 THYMIDINE ANALOGS ACTIVE AGAINST HUMAN-IMMUNODEFICIENCY-VIRUS [J].
MANSURI, MM ;
HITCHCOCK, MJM ;
BUROKER, RA ;
BREGMAN, CL ;
GHAZZOULI, I ;
DESIDERIO, JV ;
STARRETT, JE ;
STERZYCKI, RZ ;
MARTIN, JC .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1990, 34 (04) :637-641
[8]  
MARK V, 1969, TOPICS PHOSPHORUS CH, V5
[9]   TRANSESTERIFICATION REACTIONS YIELD NOVEL MASKED PHOSPHATE DERIVATIVES OF THE ANTICANCER AGENT ARAC [J].
MCGUIGAN, C ;
JONES, BCNM ;
RILEY, PA .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1991, 1 (11) :607-&
[10]   SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME PHOSPHATE TRIESTER DERIVATIVES OF THE ANTI-VIRAL DRUG ARAA [J].
MCGUIGAN, C ;
TOLLERFIELD, SM ;
RILEY, PA .
NUCLEIC ACIDS RESEARCH, 1989, 17 (15) :6065-6075