| Autor: |
Baker, B.R., Ho, Beng-Thong, Lourens, Gerhardus J. |
| Zdroj: |
Journal of Pharmaceutical Sciences; June 1967, Vol. 56 Issue: 6 p737-742, 6p |
| Abstrakt: |
A series of l-phenyl-4, 6-diamino-1,2-dihydro-2, 2-dimethyl-s-triazines (IV) bearing a phenylalkyl group on the m- or p-position of the 1-phenyl moiety was synthesized for enzymic evaluation with dihydrofolic reductase. The largest increment in binding was observed with a m-phenylbuty1 group (XIV) which gave a fortyfold increment in binding; activity was not increased by substitution of one or two chlorines on the terminal phenyl group. The most active compound (XIV) was complexed one-third as well as the potent aminopterin, that is, XIV had 95 per cent of the free energy of binding shown by aminopterin. The potential use of XIV and related compounds for treatment of tumors with an impaired active-transport system for folic acid and aminopterin is discussed. |
| Databáze: |
Supplemental Index |
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