title: Synthesis and antitumor activity of benzimidazolyl-1,3,5-triazine and benzimidazolylpyrimidine derivatives.
abstract: 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.
authors.affiliation: Research Laboratory, Zenyaku Kogyo Co, Ltd, Tokyo, Japan. Toshiyuki_Matsuno@mail.zenyaku.co.jp
authors.forename: T
authors.initials: T
authors.lastname: Matsuno
authors.forename: M
authors.initials: M
authors.lastname: Karo
authors.forename: H
authors.initials: H
authors.lastname: Sasahara
authors.forename: T
authors.initials: T
authors.lastname: Watanabe
authors.forename: M
authors.initials: M
authors.lastname: Inaba
authors.forename: M
authors.initials: M
authors.lastname: Takahashi
authors.forename: S I
authors.initials: SI
authors.lastname: Yaguchi
authors.forename: K
authors.initials: K
authors.lastname: Yoshioka
authors.forename: M
authors.initials: M
authors.lastname: Sakato
authors.forename: S
authors.initials: S
authors.lastname: Kawashima
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D047072:Aromatase Inhibitors; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D014227:Triazines / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; D004791:Enzyme Inhibitors; D011743:Pyrimidines; D014227:Triazines