SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 2-DESAMINO AND 4-DEOXY ANALOGS OF 5,10-DIDEAZATETRAHYDROFOLIC ACID (DDATHF)

被引:8
作者
SHIH, C
HU, Y
GOSSETT, LS
HABECK, LL
MENDELSOHN, LG
GRINDEY, GB
机构
[1] Lilly Research Laboratories, ELi Lilly and Company, Indianapolis
关键词
D O I
10.1016/S0960-894X(01)80736-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Either the 2-amino or the 4-oxo group of the potent GAR formyltransferase inhibitor 5,10-dideazatetrahydrofolic acid (DDATHF) was replaced with a hydrogen atom and their biological activity evaluated.
引用
收藏
页码:2657 / 2660
页数:4
相关论文
共 12 条
[1]   STRUCTURES OF APO AND COMPLEXED ESCHERICHIA-COLI GLYCINAMIDE RIBONUCLEOTIDE TRANSFORMYLASE [J].
ALMASSY, RJ ;
JANSON, CA ;
KAN, CC ;
HOSTOMSKA, Z .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (13) :6114-6118
[2]  
BALDWIN S W, 1990, Proceedings of the American Association for Cancer Research Annual Meeting, V31, P341
[3]   STRUCTURAL FEATURES OF 5,10-DIDEAZA-5,6,7,8-TETRAHYDROFOLATE THAT DETERMINE INHIBITION OF MAMMALIAN GLYCINAMIDE RIBONUCLEOTIDE FORMYLTRANSFERASE [J].
BALDWIN, SW ;
TSE, A ;
GOSSETT, LS ;
TAYLOR, EC ;
ROSOWSKY, A ;
SHIH, C ;
MORAN, RG .
BIOCHEMISTRY, 1991, 30 (07) :1997-2006
[4]  
BEARDSLEY G P, 1986, P953
[5]  
BEARDSLEY GP, 1986, P AM ASSOC CANC RES, V27, P259
[6]  
BEARDSLEY GP, 1989, J BIOL CHEM, V264, P328
[7]   CRYSTAL-STRUCTURE OF GLYCINAMIDE RIBONUCLEOTIDE TRANSFORMYLASE FROM ESCHERICHIA-COLI AT 3.0 ANGSTROM RESOLUTION - A TARGET ENZYME FOR CHEMOTHERAPY [J].
CHEN, P ;
SCHULZEGAHMEN, U ;
STURA, EA ;
INGLESE, J ;
JOHNSON, DL ;
MAROLEWSKI, A ;
BENKOVIC, SJ ;
WILSON, IA .
JOURNAL OF MOLECULAR BIOLOGY, 1992, 227 (01) :283-292
[8]  
ELLINGWOOD B, 1989, ENG J AISC, V26, P1
[9]   HETEROLOGOUS EXPRESSION AND PURIFICATION OF ACTIVE HUMAN PHOSPHORIBOSYLGLYCINAMIDE FORMYLTRANSFERASE AS A SINGLE DOMAIN [J].
KAN, CC ;
GEHRING, MR ;
NODES, BR ;
JANSON, CA ;
ALMASSY, RJ ;
HOSTOMSKA, Z .
JOURNAL OF PROTEIN CHEMISTRY, 1992, 11 (05) :467-473
[10]  
SHIH C, 1988, P AM ASSOC CANC RES, V29, P283