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Chemical Compound Review:

Fragment 20 quinazoline-2,4-diamine

Synonyms: CHEMBL268354, SureCN269636, ACMC-1BTZM, AG-E-38673, SureCN3418278, ...

Clancy, J. et al., Hunt, W.E. et al., Ommeh, S. et al., O'Dwyer, P.J. et al., Ratnam, S. et al., et al.

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Disease relevance of NSC 403373

The identification of a novel inhibitor, a 2,4-diaminoquinazoline, confirmed that such assays are useful for the detection of human immunodeficiency virus type 1 receptor antagonists [1].

High impact information on NSC 403373

In vitro activities of 2,4-diaminoquinazoline and 2,4-diaminopteridine derivatives against Plasmodium falciparum [2].
A 2,4-diaminoquinazoline, CP-101,816-1, was found to inhibit this interaction (50% inhibitory concentration in ELISA, 32.5 micrograms/ml) and to interact more strongly with CD4 than with gp120 in the consumption assays [1].
Antileishmanial activities of 2,4-diaminoquinazoline putative dihydrofolate reductase inhibitors [3].
Atomic co-ordinates, thermal parameters, bond distances and bond angles for cycloguanil and 2,4-diaminoquinazoline have been deposited as Supplementary Publication SUP 50108 (13 pages) at the British Library Lending Division, Boston Spa [4].
Trimetrexate, a 2,4-diaminoquinazoline derivative, is a new antifol recently introduced into clinical trials [5].

Gene context of NSC 403373

However, certain 2,4-diaminoquinazoline derivatives were very potent inhibitors of the plant DHFR [6].

References

Assays to detect and characterize human immunodeficiency virus type 1 (HIV-1) receptor antagonists, compounds that inhibit binding of the HIV-1 surface glycoprotein, gp120, to the CD4 receptor on human T lymphocytes. Clancy, J., Tait-Kamradt, A., Petitpas, J., Manousos, M., McGuirk, P.R., Subashi, T., Watts, P., Wondrack, L. Antimicrob. Agents Chemother. (1994) [Pubmed]
In vitro activities of 2,4-diaminoquinazoline and 2,4-diaminopteridine derivatives against Plasmodium falciparum. Ommeh, S., Nduati, E., Mberu, E., Kokwaro, G., Marsh, K., Rosowsky, A., Nzila, A. Antimicrob. Agents Chemother. (2004) [Pubmed]
Antileishmanial activities of 2,4-diaminoquinazoline putative dihydrofolate reductase inhibitors. Berman, J.D., King, M., Edwards, N. Antimicrob. Agents Chemother. (1989) [Pubmed]
Crystallographic and molecular-orbital studies on the geometry of antifolate drugs. Hunt, W.E., Schwalbe, C.H., Bird, K., Mallinson, P.D. Biochem. J. (1980) [Pubmed]
Trimetrexate: a new antifol entering clinical trials. O'Dwyer, P.J., Shoemaker, D.D., Plowman, J., Cradock, J., Grillo-Lopez, A., Leyland-Jones, B. Investigational new drugs. (1985) [Pubmed]
Purification and characterization of dihydrofolate reductase from soybean seedlings. Ratnam, S., Delcamp, T.J., Hynes, J.B., Freisheim, J.H. Arch. Biochem. Biophys. (1987) [Pubmed]

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