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J Med Chem. 1993 Oct 29;36(22):3464-71.

Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some sulfonamidobenzoylglutamate and related derivatives.

Author information

1
Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709.

Abstract

Several folate-like thymidylate synthase inhibitors are described in which the pteridine nucleus of the folic acid molecule is replaced by a benzoquinazoline moiety, which in turn is attached to the benzoylglutamate side chain by a sulfonamide link. The most potent compounds had Ki values as low as 2.5 nM against the human enzyme, were good substrates for the cellular reduced folate transport system and for folylpolyglutamate synthetase, and had IC50 values for growth inhibition of tumor cell lines as low as 70 nM.

PMID:
8230138
DOI:
10.1021/jm00074a030
[Indexed for MEDLINE]

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