TY - JOUR
T1 - Synthesis and biological activity of 1,3,5-triazino[1,2-a]benzimidazol-2- amines
AU - Dolzhenko, A. V.
AU - Chui, W. K.
N1 - Copyright:
Copyright 2009 Elsevier B.V., All rights reserved.
PY - 2007/9
Y1 - 2007/9
N2 - 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).
AB - 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).
UR - http://www.scopus.com/inward/record.url?scp=40049100801&partnerID=8YFLogxK
U2 - 10.1007/s11094-007-0103-5
DO - 10.1007/s11094-007-0103-5
M3 - Article
AN - SCOPUS:40049100801
VL - 41
SP - 470
EP - 473
JO - Pharmaceutical Chemistry Journal
JF - Pharmaceutical Chemistry Journal
SN - 0091-150X
IS - 9
ER -