engleski

Novel 5-amidino benzimazoles as selective cytostatic agents against lung cancer cells

Lung cancer is one of the most common malignant tumors in the world. Dysregulation of p38 mitogenactivated protein kinase (MAPK) levels in patients are associated with advanced stages and short survival in cancer patients (e.g., prostate, breast, bladder, liver, and lung cancer) [1]. The benzimidazole derivatives have shown various biological activities such as anticancer, antimicrobial, antivirus, anti- inflammatory and antioxidant [2]. Moreover, the amidino moiety is among the strongest neutral bases with high proton affinity and has therefore found wide application in biologically active compounds [3]. We designed and synthesized novel 1, 2, 3-triazolyl linked 5- amidino benzimidazoles (Figure 1) in order to evaluate their cytostatic activities. Environmentally benign synthetic protocols using microwave- and ultrasound irradiation were used to prepare 1, 4- disubstituted-1, 2, 3-triazoles, as key precursors in the synthesis of novel 5-amidino benzimidazoles. Some representatives have shown selective inhibitory effects against non-small lung carcinoma (A-549) and cervical carcinoma (HeLa). Further biological evaluations of the most selective compounds indicated their mechanism of action via the p38 MAP kinase pathway.

amidino benzimidazoles ; 1, 2, 3-triazoles ; lung carcinoma ; p38MAPK

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