Synthesis and anticancer activity evaluation of substituted carbazole bearing thiosemicarbazide derivatives against human glioma U87 MG cell line
Neuro-pharmaceutical Research Laboratory, Dr. BR. Ambedkar Centre for Biomedical Research (ACBR), University of Delhi, 110007, India.
Research Article
World Journal of Advanced Research and Reviews, 2022, 16(03), 884-892
Article DOI: 10.30574/wjarr.2022.16.3.1402
Publication history:
Received on 11 November 2022; revised on 21 December 2022; accepted on 24 December 2022
Abstract:
Both carbazole and thiosemicarbazide scaffold showed various potential biological activities in medicinal chemistry. In this research work, we synthesized a series of carbazole bearing thiosemicarbazide derivatives (17-28) and evaluated thier in vitro cytotoxicity (IC50) profile on the U87 MG cell line using MTT assay. All target compounds were well characterized by NMR and HRMS mass spectroscopy. In series, six compounds (17, 20, 21, 22, 23, 28) found better in vitro cytotoxicity (IC50) values were 26.50 µM, 34.0 µM, 39 µM, 80 µM, 62 µM, 50 µM respectively compare to standard drug Temozolomide (IC50 = 100 µM). The SAR study of all final compounds (17-28) were also analyzed on the basis of different substituents on 6th position of carbazole scaffold bearing thiosemicarbazide derivatives against U87 MG cell line. All of the above studies showed that carbazole bearing thiosemicarbazide derivatives (17-28) showed anticipated anticancer activity against U87 MG glioma cell line.
Keywords:
GBM (Glioblastoma); Carbazole; Thiosemicarbazide; TMZ (Temozolomide); Compound 17((E)-2-((1,4-dimethyl-9-H-carbazol-3-yl)methylene)hydrazinecarbothioamide); SAR (Structure activity relationship); MTT (tetrazolium salt (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)
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