Kodisundaram P, Duraikannu A, Balasankar T, Sundarao Ambure P, Roy K. Cytotoxic and Antioxidant Activity of a Set of Hetero Bicylic Methylthiadiazole Hydrazones: A Structure-Activity Study. Int J Mol Cell Med 2015; 4 (2) :128-137
URL:
http://ijmcmed.org/article-1-261-en.html
1- Department of Chemistry, Annamalai University, Annamalai Nagar-608002, Tamilnadu, India.
2- Department of Clinical Neurosciences, University of Calgary, Calgary, Alberta T2N 4N1, Canada.
3- Chemistry section, FEAT, Annamalai University, Annamalai nagar-608002, Tamilnadu, India. , kdsundaram1@gmail.com
4- Drug Theoretics and Cheminformatics Laboratory, Department of Pharmaceutical Technology, Jadavpur University, Jadavpur, Kolkata, 700032, India.
5- Manchester Institute of Biotechnology, University of Manchester, Manchester M1 7DN, Great Britain.
Abstract: (11381 Views)
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.
Type of Study:
Original Article |
Subject:
Cancer Received: 2014/11/12 | Accepted: 2015/02/18 | Published: 2015/05/12