Synthesis, antimycobacterial and anticancer activity of novel indole-based thiosemicarbazones

被引:0
作者
Vida Mashayekhi
Kamaleddin Haj Mohammad Ebrahim Tehrani
Parisa Azerang
Soroush Sardari
Farzad Kobarfard
机构
[1] Zanjan University of Medical Sciences,Department of Pharmaceutical Biotechnology, School of Pharmacy
[2] Zanjan University of Medical Sciences,Department of Medicinal Chemistry, School of Pharmacy
[3] Pasteur Institute,Drug Design and Bioinformatics Unit, Department of Medical Biotechnology, Biotechnology Research Center
[4] Shahid Beheshti University of Medical Sciences,Department of Medicinal Chemistry, School of Pharmacy
[5] Shahid Beheshti University of Medical Sciences,Phytochemistry Research Center
来源
Archives of Pharmacal Research | 2021年 / 44卷
关键词
1-Substituted indole-3-carboxaldehydes; Thiosemicarbazone; Antimycobacterial activity; Anticancer; MTT assay;
D O I
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学科分类号
摘要
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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页码:1 / 13
页数:12
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