alexa Abstract | Design, Synthesis, Characterization and Anticancer Properties of Novel 2-Chloro-N-(Aryl Substituted) Acetamide Derivatives of 5-[2-(4- Methoxyphenyl) Pyridin-3-yl]-1, 3, 4-Oxadiazole-2-Thiol

International Journal of Drug Development and Research
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Abstract

In this linear synthesis, novel different 2-chloro N-aryl substitutedacetamide derivatives of 5-[2-(4-methoxyphenyl) pyridin-3-yl]-1, 3, 4-oxadiazole-2-thiol have been synthesized and screened for their cytotoxicity on PANC-1, HepG2 and MCF7 cell lines and obtained the IC50 and CC50 values.All the synthesized compounds were characterized by LCMS, IR, 1H and 13C (proton and Carbon 13) spectroscopies and elemental analysis. These compounds were evaluated for invitro anticancer activity on three different human leukemic cell lines, namely PANC-1,HepG2 and MCF7.In total five compounds were synthesized and studied for their MTT assay. Among five synthesized novel compounds, the compound N- [5-(4-Methoxy-phenyl)-pyridin-2-yl]-2-{5-[2-(4-methoxy-phenyl)-pyridin-3- yl][1,3,4]oxadiazol-2-ylsulfanyl}-acetamide6e is highly cytotoxic on PANC-1 and HepG2 cell lines having IC50 of 4.6μM and 2.2μM respectively whereas the compound 6c is moderately cytotoxic on MCF7 having IC50 15.5μM respectively. Rest all the compounds showed less cytotoxicity on all the three cell lines as compared with the standard 5-FU.

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Author(s): Adimule Vinayak Medapa Sudha Kumar S lalita Rao Prakash Kumar

Keywords

HepG2, 1, 3, 4-Oxadiazoles, Chloroacetyl chloride, acetamide, MTT assay

 
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