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KMID : 0043320210440080764
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Archives of Pharmacal Research
2021 Volume.44 No. 8 p.764 ~ p.776
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Synthesis, antimycobacterial and anticancer activity of novel indole-based thiosemicarbazones
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Mashayekhi Vida
Tehrani Kamaleddin Haj Mohammad Ebrahim
Azerang Parisa
Sardari Soroush
Kobarfard Farzad
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Abstract
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Based on the structural elements of bioactive indole-based compounds, a series of novel 1-substituted indole-3-carboxaldehyde thiosemicarbazones were synthesized as potential antimycobacterial and anticancer agents. The derivatives were prepared via a two-step methodology including N-alkylation(benzylation) of indole-3-carboxaldehyde and conversion of the intermediate aldehydes to corresponding thiosemicarbazones. The derivatives were evaluated for their antimycobacterial activity and compounds 3d (R = propyl) and 3q (R = 4-nitrobenzyl) were among the most potent and selective derivatives with IC50 values of 0.9 and 1.9 μg/mL respectively. The anticancer activity of the derivatives was also assessed against a panel of tumor cell lines. Compounds 3t, 3u, 3v and 3w efficiently inhibited the majority of the cancer cell lines with considerable selectivity.
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KEYWORD
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1-Substituted indole-3-carboxaldehydes, Thiosemicarbazone, Antimycobacterial activity, Anticancer, MTT assay
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