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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Evaluation of Certain Symmetrical Schiff Bases as Inhibitors of MDA-MB-241 Human Breast Cancer Cell Proliferation

Author(s): Smaail Radi, Said Tighadouini, Olivier Feron, Olivier Riant and Yahia N. Mabkhot

Volume 13 , Issue 3 , 2016

Page: [205 - 209] Pages: 5

DOI: 10.2174/1570180812999150812165510

Price: $65


A series of symmetrical Schiff base derivatives (L1-L7) were designed by a one-pot condensation reaction of various aldehyde/ketone compounds with hydrazine under mild conditions (room temperature, 3 days), using ether as solvent and acetic acid as catalyst. The target products were characterized and analysed by 1H and 13C NMR, FT-IR and liquid chromatography mass spectrometry (LC/MS). Our research focuses on the identification of synthetically chemotherapeutic substances able to inhibit, delay, or reverse the process of carcinogenesis in several stages. The target compounds presenting two regions for SAR evaluation were screened for their activity toward MDA-MB-241 breast cancer cell proliferation for the first time. Compound (1E, 2E)-1,2-bis(1-(3-nitrophenyl)ethylidene) hydrazine (L6) showed significant inhibitory activity (IC50 = 7.08 µg/mL).

Keywords: Schiff bases, heterocycles, nitro, antitumor activity, breast cancer, cell proliferation.

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