Author:
Abbas Hebat-Allah S.,Nossier Eman S.,El-Manawaty May A.,El-Bayaa Mohamed N.
Abstract
AbstractNew sulfonamide-triazole-glycoside hybrids derivatives were designed, synthesised, and investigated for anticancer efficacy. The target glycosides’ cytotoxic activity was studied with a panel of human cancer cell lines. Sulfonamide-based derivatives, 4, 7 and 9 exhibited promising activity against HepG-2 and MCF-7 (IC50 = 8.39–16.90 μM against HepG-2 and 19.57–21.15 μM against MCF-7) comparing with doxorubicin (IC50 = 13.76 ± 0.45, 17.44 ± 0.46 μM against HepG-2 and MCF-7, rescpectively). To detect the probable action mechanism, the inhibitory activity of these targets was studied against VEGFR-2, carbonic anhydrase isoforms hCA IX and hCA XII. Compoumds 7 and 9 gave favorable potency (IC50 = 1.33, 0.38 μM against VEGFR-2, 66, 40 nM against hCA IX and 7.6, 3.2 nM against hCA XII, respectively), comparing with sorafenib and SLC-0111 (IC50 = 0.43 μM, 53 and 4.8 nM, respectively). Moreover, the docking simulation was assessed to supply better rationalization and gain insight into the binding affinity between the promising derivatives and their targeted enzymes that was used for further modification in the anticancer field.
Funder
National Research Centre Egypt
Publisher
Springer Science and Business Media LLC
Reference73 articles.
1. Esfandiari, M. K., Baharloui, M., Houshdar, T. M. H., Mirshokraee, S. A. & Balalaie, S. The synthesis of conjugated peptides containing triazole and quinolone-3- carboxamide moieties designed as anticancer agents. Iran. J. Biotechnol. 19(4), 83–91 (2021).
2. Alotabi, S. H. Synthesis, characterization, anticancer activity, and molecular docking of some new sugar hydrazone and arylidene derivatives. Arab. J. Chem. 13(3), 4771–4784 (2020).
3. Batchelor, D. Hair and cancer chemotherapy: Consequences and nursing care e a literature study. Eur. J. Cancer Care. 10(3), 147–163 (2001).
4. Reiche, E. M. V., Nunes, S. O. V. & Morimoto, H. K. Stress, depression, the immune system, and cancer. Lancet Oncol. 5(10), 617–625 (2004).
5. Bukowski, K., Kciuk, M. & Kontek, R. Mechanisms of multidrug resistance in cancer chemotherapy. Int. J. Mol. Sci. 21(9), 3233 (2020).
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