Anticancer effect of three pyrazole derivatives.
The evaluation of the cytotoxic properties in vitro of three synthetic tripods containing pyrazole: N,N-bis[(3,5-dimethylpyrazol-1-yl)methyl]aniline (1); N,N-tetrakis[(3,5-dimethylpyrazol-1-yl)methyl]-para-phenylenediamine (2); and N,N-tetrakis-[(1,5-dimethylpyrazol-3-yl)methyl]-para-phenylenediamine (3), was examined for their cytotoxic activity on two tumor cell lines: P815 (murin mastocytoma) and Hep (human laryngeal carcinome). While the compound 2 shows a small cytotoxic activity, compounds 1 and 3 are more cytotoxic against both cell lines. However, this cytotoxicity is more pronounced against Hep cell line (IC50: 3.25 microg mL(-1) for compound 1 and 6.92 microg mL(-1) for compound 3) than P815 cell line (IC50: 17.82 microg mL(-1) for compound 1 and 37.21 microg mL(-1) for compound 3). Statistical analysis shows that the compound 1 is two- to threefold more cytotoxic than compound 3 (P < 0.05). Interestingly, the cytotoxicity induced by compound 1 against Hep cell line is more important than that induced by adriamycin used as a positive control.
Bouabdallah
Ibrahim
I
Laboratory of Organic Chemistry, Macromolecular and Natural Products, Faculty of Sciences, University Mohammed Ier, BP 524, 60 000 Oujda, Morocco.
M'Barek
Lahcen Ait
LA
Zyad
Abdelmajid
A
Ramdani
Abdelkrim
A
Zidane
Ismail
I
Melhaoui
Ahmed
A
D000814:Aniline Compounds / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D015394:Molecular Structure; D010655:Phenylenediamines / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology*
D000814:Aniline Compounds; D000970:Antineoplastic Agents; C515764:N,N-bis((3,5-dimethylpyrazol-1-yl)methyl)aniline; C515765:N,N-tetrakis((3,5-dimethylpyrazol-1-yl)methyl)-para-phenylenediamine; D010655:Phenylenediamines; D011720:Pyrazoles