29419-15-6Relevant articles and documents
FUSED IMIDAZOLE DERIVATIVE
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Page 8, (2008/06/13)
According to the present invention, fused imidazole derivatives of the general formula: wherein R1 is a hydrogen atom, a halogen atom, hydroxy group, a lower alkyl group or a lower alkoxy group, R2 is an aryl group, benzodioxanyl group, or 5-6 membered, monocyclic, unsaturated, heterocyclic group containing nitrogen atom(s) which may be substituted with lower alkyl, trityl or oxo, R3 is a hydrogen atom or hydroxy group, A is a group represented by the formula : -(CH2)m - or -O-(CH2)m- [wherein m is an integer of 1-3] and their salts are provided.
Benzoquinazoline inhibitors of thymidylate synthase: Enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin- 1(2H)-ones
Pendergast,Johnson,Dickerson,Dev,Duch,Ferone,Hall,Humphreys,Kelly,Wilson
, p. 2279 - 2291 (2007/10/02)
The synthesis and thymidylate synthase (TS) inhibitory activity of a series of simple benzo[f]-quinazolin-1(2H)-ones are described. Fully aromatic 3-amino compounds with compact lipophilic substituents in the 9-position were found to have I50 values as low as 20 nM on the isolated enzyme, and represent the first examples of potent, folate-based TS inhibitors that completely lack any structural feature corresponding to the (p- aminobenzoyl)glutamate moiety of the cofactor. A number of the compounds also showed moderate growth inhibitory activity against a human colon adenocarcinoma cell line (SW480), with IC50 values as low as 2 μM.