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5,8-dideazaisofolic acid
structure given in first source
Also Known As:
5,8-dideazaisopteroylglutamate; IAHQ
Networked:
8
relevant articles (
0
outcomes,
1
trials/studies)
Bio-Agent Context: Research Results
Heterocyclic Compounds: 198
Fused-Ring Heterocyclic Compounds
2-Ring Heterocyclic Compounds
Quinazolines: 402
5,8-dideazaisofolic acid: 8
Related Diseases
1.
Osteosarcoma (Osteogenic Sarcoma)
01/01/1982 - "
For in vivo studies, human osteosarcoma (OS) cells from the IAHQ-sensitive line TE-85 were implanted intraperitoneally in newborn hamsters: in the group treated with IAHQ, only 30% of the animals developed OS, compared with 100% of those not treated with IAHQ.
"
01/01/1986 - "
The folate analogue 5,8-dideazaisopteroylglutamate (IAHQ; NSC-289517) inhibits the growth of a variety of human tumor cells in vitro such as colon, breast and osteosarcoma.
"
2.
Neoplasms (Cancer)
01/01/1986 - "
The results suggest that probenecid could be used to enhance the effectiveness of IAHQ against solid tumors such as colon adenocarcinoma.
"
04/01/1986 - "
However, in tumor cells incubated with growth-inhibitory concentrations of either FdUrd or 5,8-dideazaisofolic acid for 48 h, the rate of thymidylate synthase activity was between 15- and 17-fold greater than the rate of DNA synthesis.
"
01/01/1982 - "
Effects of 5,8-dideazaisofolic acid (IAHQ) on human tumor cells in culture and on normal and tumor-bearing hamsters.
"
01/01/1983 - "
Of the quinazolines tested, 5,8-dideazaisopteroylglutamate, (IAHQ), when administered at 85 mg/kg on days 2 and 10 after tumor implantation delayed the growth of colon tumor No. 38, and resulted in 6 of 20 tumor-free animals at 90 days.
"
01/01/1986 - "
The folate analogue 5,8-dideazaisopteroylglutamate (IAHQ; NSC-289517) inhibits the growth of a variety of human tumor cells in vitro such as colon, breast and osteosarcoma.
"
3.
Colonic Neoplasms (Colon Cancer)
01/01/1983 - "
IAHQ was also active against human colon adenocarcinoma cells (HCT-8) in tissue culture, requiring a concentration of 5 X 10(-7) M to inhibit cell growth 50% after 72 hours continuous exposure.
"
01/01/1986 - "
The results suggest that probenecid could be used to enhance the effectiveness of IAHQ against solid tumors such as colon adenocarcinoma.
"
01/01/1983 - "
Effects of 5,8-dideazaisopteroylglutamate and its possible tri-gamma-glutamyl metabolite (5,8-dideazaisoPteGlu3) on colon adenocarcinoma, and the folate dependent enzymes thymidylate synthase and dihydrofolate reductase.
"
03/15/1988 - "
The uptake and metabolism of radiolabeled 5,8-dideazaisofolic acid (IAHQ) (N-[p- ([(2-amino-4-hydroxy-6-quinazolinyl)amino]methyl)benzoyl]-L-glutamic acid), a new antifol targeted to thymidylate synthase, has been investigated in the human colon adenocarcinoma cell line HCT-8.
"
01/01/1983 - "
Chief among these are 5,8-dideazaisopteroylglutamate, 5,8-dideazaisoPteGlu, (IAHQ), a compound with proven activity against the growth of human colon adenocarcinoma cells in vitro, and 10-formyl-5,8-dideazapteroylglutamic acid, which serves as a substrate for glycinamide ribonucleotide transformylase and is also an effective inhibitor of mammalian thymidylate synthase.
"
4.
Carcinoma (Carcinomatosis)
03/15/1988 - "
Uptake and metabolism of 5,8-dideazaisofolic acid in human colon carcinoma cells.
"
11/15/1987 - "
Mechanism of action of 5,8-dideazaisofolic acid and other quinazoline antifols in human colon carcinoma cells.
"
5.
Leukemia L1210
01/01/1986 - "
Since IAHQ has only modest activity against L1210 leukemia in mice, it was tested in combination with methotrexate (MTX), probenecid, or verapamil in an effort to enhance efficacy.
"
01/01/1986 - "
Effects of 5,8-dideazaisopteroylglutamate (IAHQ) on L1210 leukemia in mice when given alone and in combination with methotrexate, probenecid, or verapamil.
"
Related Drugs and Biologics
1.
5,8-dideazaisofolic acid
2.
Thymidylate Synthase
3.
Quinazolines
4.
Folic Acid (Vitamin M)
5.
Methotrexate (Mexate)
6.
Phosphoribosylglycinamide Formyltransferase
7.
Glutamic Acid (Glutamate)
8.
Trimetrexate (JB11)
9.
Verapamil (Calan)
10.
Tetrahydrofolate Dehydrogenase (Dihydrofolate Reductase)