Anticancer effect of three pyrazole derivatives

Abstract

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.

Crystal structure of ethyl-5-amino-1-(2,4-dinitrophenyl)-1H-pyrazole-4-carboxylate, C12H11N5O6

“…The nest labeled possessions of virtually all group of pyrazoles is in the handling of swelling and swelling allied complaints, for example arthritis [2]. They are the theme of numerous exploration revisions owing to their rife impending biotic accomplishments for instance uncontaminated [3], antiviral, anticancer [4][5][6], antihistaminic, antidepressant [7,8], and antifungal activity [9]. More than a few pyrazole spino s have been recruiting to retain noteworthy goings-on for instance 5-α-red-uctase inhibitor [9].…”

Synthesis of New Heterocyclic Compounds with Biological Activity against Pathogenic Microbes in the Albaha Area

“…The most common use for pyrazoles is to treat inflammation and inflammation-associated disorders such as arthritis [2]. Pyrazole derivatives are the subject of many studies due to their potential antimicrobial [3], Antiviral [4], Antitumor [5,6], Antihistaminic [7], Antidepressant [8], Insecticidal and fungicidal properties [9]. Pyrazole derivatives function as 5-α-reductase inhibitors [10].…”

Synthesis of Some Novel Heterocyclic and Schiff Base Derivatives as Antimicrobial Agents

“…The reaction of such compounds with nitrogen and carbon nucleophiles produces many biologically active heteocyclic compounds. For example, substituted pyrazoles are reported to be an important class of compounds in the agricultural and medicinal chemistry fields because of their broad spectrum biological activities [3][4][5][6] and they also have anti-cancer effects [7]. Imidazole derivatives act as potent and selective neuropeptide Y Y5 receptor antagonists, having antifungal and antibacterial activity and are used as potential tuberculostatic agents [8][9][10].…”