Chemical and Pharmaceutical Bulletin
Synthesis and Antitumor Activity of Benzimidazolyl-1, 3, 5-triazine and Benzimidazolylpyrimidine Derivatives
Toshiyuki MATSUNOMasanobu KATOHiroya SASAHARATetsuo WATANABEMasahiro INABAMasayuki TAKAHASHIShin-ichi YAGUCHIKimitomo YOSHIOKAMitsuo SAKATOSeiichiro KAWASHIMA
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Volume 48 (2000) Issue 11 Pages 1778-1781

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Abstract

Triamino-substituted 1, 3, 5-triazine and pyrimidine derivatives were synthesized and tested for antimtuor 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-traizine 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.

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© The Pharmaceutical Society of Japan
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