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Triamino-substituted 1,3,5-triazine and pyrimidine derivatives were synthesized and tested for antitumor activities using some human cancer cell lines and murine leukemia cell lines. All the compounds having benzimidazolyl and morpholino groups as substituents on the 1,3,5-triazine ring showed antitumor activity. Pyrimidine derivatives having the same groups as substituents also showed antitumor activity. Among them, the compounds having 1-benzimidazolyl, morpholino and cis-2,3-dimethylmorpholino groups as substituents on the 1,3,5-triazine ring or pyrimidine ring exhibited the most potent antitumor activity, and these compounds exhibited no or very weak aromatase inhibitory activity. In contrast, the compounds having imidazolyl group instead of benzimidazolyl group as a substituent on the 1,3,5-triazine ring showed a potent aromatase inhibitory activity.
Nine condensed tannin related compounds isolated from LINDERAE UMBELLATAE Ramus, (+)-catechin ( 1), (-)-epicatechin ( 2), proanthocyanidin B-1 ( 3), B-2 ( 4), B-4 ( 5), trimer A ( 6), trimer B ( 7), cinnamtannin B (1) ( 8) and cinnamtannin D (1) ( 9), were tested for their effects on peptic activity and stress-induced gastric lesions in mice. Peptic activity of rat gastric juice was suppressed by 6 and 7 IN VITRO, and slightly suppressed by 8 and 9. In pylorus-ligated mice, these compounds, except for 4, administered orally exhibited anti-peptic activity. Pretreatments of 4,6 and 7 orally protected mice against stress-induced gastric lesions. Effects of these compounds on digestive systems were dìscussed.
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