Kesuma, Dini and ., Siswandono and Purwanto, Bambang Tri and Rudyanto, Marcellino (2018) Synthesis of N-(phenylcarbamothioyl)-benzamide derivatives and their cytotoxic activity against MCF-7 cells. Journal of Chinese Pharmaceutical Sciences, 27 (10). pp. 696-702. ISSN 1003-1057
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Abstract
Cancer is one of the leading causes of death both in developing countries and across the globe. In Indonesia, cancer ranks as the fifth primary cause of death following heart disease, stroke, respiratory tract and diarrhea. Therefore, studies on thiourea derivative compounds as anticancer agents have been profoundly conducted but still require further continuous development. In the present study, we aimed to synthesize new anticancer compounds of N-(phenylcarbamothioyl)-benzamide derivatives, namely N-(phenylcarbamothioyl)-4-bromobenzamide and N-(phenylcarbamothioyl)-4-fluorobenzamide compounds and assess their activities against MCF-7 breast cancer cells. The initial step was to predict the drug-receptor activity through docking between the tested compounds using epidermal growth factor receptor (EGFR) (PDB code: 1M17). The compounds were futher synthesized from the reactions between benzoyl chloride derivatives and N-phenylthiourea. The structures of the new compounds were identified using FTIR, 1H NMR, 13C NMR and mass spectra. The cytotoxic activities (IC50) to breast cancer cells of MCF-7 N-(phenylcarbamothioyl)-4-bromobenzamide compound and N-(phenylcarbamothioyl)-4-fluorobenzamide were 0.27 mM and 0.31 mM, respectively. These two new compounds had better cytotoxic activities than those of the current hydroxyurea-based anticancer drugs (the reference compound) with an IC 50 value of 9.76 mM. Furthermore, these two new compounds were not toxic to Vero normal cells. Therefore, they possessed tremendous potentials as the candidates for new drugs against breast cancer.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | N-(phenylcarbamothioyl)-benzamide derivatives; Cytotoxic; MCF-7 cells; EGFR |
| Subjects: | R Medicine > RS Pharmacy and materia medica |
| Divisions: | Faculty of Pharmacy > Department of Pharmacy |
| Depositing User: | Ester Sri W. 196039 |
| Date Deposited: | 08 Nov 2018 05:12 |
| Last Modified: | 24 Mar 2021 15:57 |
| URI: | http://repository.ubaya.ac.id/id/eprint/33833 |
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