Abstract
Abstract This paper reports the synthesis and in vitro cytotoxicity evaluation of isatin-pyrrole derivatives 5–8, obtained from the appropriate isatins with pyrrole, with good yields and purity. The product structures were confirmed through spectroscopy methods. Furthermore, the MTT assay on the human liver cancer HepG2 cell lines revealed moderate activity in all compounds, which was highest in sample 6 (IC50 0.47 µM). The anticancer activity was affiliated with the presence of a nitro group at C-5 and N-methyl of the isatin scaffold.
Highlights
The stock solutions of 5–8 and the doxorubicin control compound were individually combined with dimethyl sulfoxide (DMSO) and diluted serially in Roswell Park Memorial Institute (RPMI) to yield the varying concentrations (12.5, 25, 50, 100, 200, and 400 μg/mL)
(2) In 1H-nuclear magnetic resonance (NMR), the spectrum showed a singlet at 3.55 ppm which indicated methyl group protons and two doublets at 7.41 and 8.32 ppm and another doublet at 8.60 ppm for aromatic protons
A previous report [25] showed the presence of singlet signal at 3.38 ppm for methyl group protons, based on 1H-NMR data
Summary
Cancer is a serious threat to human health and a leading cause of death globally [1]. There is a need to develop drugs with lower Pyrrole is another important active chromophore with heterocyclic aromatic characteristics. It contains a nitrogen atom and is part of the cofactors and natural products of vitamin B12 and porphyrinogens [13,14]. Pyrrole possesses broad-spectrum bioactivities, including anticancer and antibacterial functions [15,16], while molecular hybrid derivatives, including oroidin and sophoridine, recently exhibited remarkable anticancer activity against MCF-7 and HepG2 cancer cell lines [15,17]. The trimethoxybenzaldehyde-pyrrole hybrid demonstrated good effects against HeLa and MCF-7 [18]. These findings suggest the need to investigate the combination of pharmacophoric elements including isatin and pyrrole, in a single chemical framework, and to investigate their cytotoxicity. Alongside with their anticancer activity against HepG2 cancer cell lines
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