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Title: Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2- amines
Authors: Dolzhenko, A.V. 
Chui, W.K. 
Issue Date: Sep-2007
Citation: Dolzhenko, A.V.,Chui, W.K. (2007-09). Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2- amines. Pharmaceutical Chemistry Journal 41 (9) : 470-473. ScholarBank@NUS Repository.
Abstract: Several 4-substituted 1,3,5-triazino[1,2-a]benzimidazol-2-amines were prepared via cyclization of 2-benzimidazolylguanidine with various reactants. The prototropic tautomerism in the obtained dihydro analogs was investigated. According to the NMR data, the 3,4-dihydro form was found to predominate in DMSO solutions. All tested compounds inhibited the activity of mammalian dihydrofolate reductase. The most active compound was 4,4-dimethyl-3,4- dihydro[1,3,5]triazino[1,2-a]benzimidazol-2-amine (IC50 = 10.9 mM). © 2007 Springer Science+Business Media, Inc.
Source Title: Pharmaceutical Chemistry Journal
ISSN: 0091150X
DOI: 10.1007/s11094-007-0103-5
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