P. Tsitsa, E. Antoniadou‐Vyza, S. Hamodrakas
Jul 27, 1993
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0
Influential Citations
14
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Quality indicators
Journal
European Journal of Medicinal Chemistry
Abstract
Abstract A number of adamantyl-group-bearing diamino- s -triazines were synthesized as potential dihydrofolate reductase (DHFR) inhibitors and their pharmacological properties were tested. The crystal structures of certain compounds were determined by X-ray crystallography. With the aid of computer graphics, model structures of the L1210 mouse DHFR-ligand ternary complex were constructed. The binding affinities of the compounds to DHFR were determined experimentally. Compounds mono-substituted at the nitrogen of the amine group appear to be slightly better inhibitors. Weak activity was also enhanced by the presence of a methylene bridge between the adamantyl group and the s -triazine ring. The majority of the compounds was shown to have weak activity against P388 and KB cell lines in vitro ; some compounds showed weak anti-bacterial activity and no anti-viral activity was detected.