In vitro cytotoxicity of imidazolyl-1,3,5-triazine derivatives.

Abstract

We examined in vitro cytotoxic activity of imidazolyl-1,3,5-triazine derivatives using human breast cancer cell lines (MCF-7, R-27, T-47D and ZR-75-1) and murine leukemia cell line (P388). The percentage of viable cells was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazorium bromide (MTT) assay. Hexamethylmelamine (HMM), a 1,3,5-triazine derivative has previously been recognized as an antitumor agent effective against lung, ovarian and breast cancer, but failed to show a significant cytotoxic activity in the present study. In contrast, four imidazolyl-1,3,5-triazine derivatives, 2-(1-imidazolyl)-4,6-bis(morpholino)-1,3,5-triazine, 2-(1-imidazolyl)-4-morpholino-6-(3-thiazolidinyl)-1,3,5-triazine, 2-(4-cyano-4-phenylpiperidino)-4-(1-imidazolyl)-6-morpholino-1,3,5-triaz ine and 2-(1-imidazolyl)-4-(N-methyl-N-phenylamino)-6-morpholino-1,3,5-triazine showed cytotoxic activity for most cell lines, which was significantly greater than the activity of hydroxymethylpentamethylmelamine (HMPMM), a major metabolite of HMM.

• Authors: S Yaguchi, Y Izumisawa, M Sato, T Nakagane, I Koshimizu, K Sakita, M Kato, K Yoshioka, M Sakato, S Kawashima
• Journal: Biological & pharmaceutical bulletin (Biol Pharm Bull) Vol. 20 Issue 6 Pg. 698-700 (Jun 1997) ISSN: 0918-6158 [Print] Japan
• PMID: 9212994 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Triazines
• 2-N,N-dimethylamino-4,6-bis(1-H-imidazol-1-yl)-1,3,5-triazine
• Fadrozole
• Altretamine

Topics

• Altretamine (analogs & derivatives, pharmacology)
• Animals
• Antineoplastic Agents (chemistry, pharmacology)
• Breast Neoplasms (pathology)
• Cell Survival (drug effects)
• Drug Screening Assays, Antitumor
• Fadrozole (pharmacology)
• Humans
• Leukemia P388 (pathology)
• Mice
• Structure-Activity Relationship
• Triazines (chemistry, pharmacology)
• Tumor Cells, Cultured