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
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Insight Medical Publishing
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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Keywords
HepG2, 1, 3, 4-Oxadiazoles, Chloroacetyl chloride, acetamide, MTT assay