cytotoxic and antioxidant activity of a set of hetero bicylic methylthiadiazole hydrazones: a structure-activity study

Authors

paulrasu kodisundaram department of chemistry, annamalai university, annamalai nagar-608002, tamilnadu, india.

arul duraikannu department of clinical neurosciences, university of calgary, calgary, alberta t2n 4n1, canada.

thirunavukkarasu balasankar chemistry section, feat, annamalai university, annamalai nagar-608002, tamilnadu, india.

pravin sundarao ambure drug theoretics and cheminformatics laboratory, department of pharmaceutical technology, jadavpur university, jadavpur, kolkata, 700032, india.

abstract

the current study highlights the in vitro antioxidant and antitumor activity of the previously-synthesized hydrazone derivatives against various free radicals and human cancer cell lines, respectively. the anticancer efficacies of the compound were tested by measuring cytotoxicity in cancer cell lines hela, a549, and non-cancerous nl20 cells. compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects. the free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis. the results from cytotoxicity and cell migration assay showed that the substitution of electron-withdrawing fluoro, chloro and bromo functional groups induced a significant (p< 0.001) loss of cell viability and inhibited the invasive potential of the human cancer cells. additionally, these compounds showed significantly (p< 0.05) a less toxicity toward non-cancerous nl20 cells. docking studies revealed interactions of compound 10 with p38α map kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

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Journal title:
international journal of molecular and cellular medicine

جلد ۴، شماره ۲، صفحات ۱۲۸-۱۳۷

Keywords
[ ' a n t i o x i d a n t ' , ' a n t i c a n c e r ' , 3 , ' a z a b i c y l o n o n e s ' , ' h y d r a z o n e s ' , ' c y t o t o x i c i t y ' ]

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