Dini Kesuma and Siswandono and Bambang Tri Purwanto and Marcellino Rudyanto (2019) Synthesis and anticancer evaluation of N-benzoyl-N’phenyltiourea derivatives againts human breast cancer cells (T47D). Journal of Chinese Pharmaceutical Sciences, 29 (2). pp. 123-129. ISSN 1003-1057

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Abstract

New anti-breast cancer compounds have been found and may prove to have stronger activity. To predict the activities of N-benzoyl-N'-phenylthiourea (BPTU) derivatives, namely N-(3-chloro)benzoyl-N'-phenylthiourea (3-Cl-BPTU) and N-(3,4-dichloro)benzoyl-N'-phenylthiourea (3,4-2Cl-BPTU) with Sirtuin-1 receptor (PDB code: 4I5I), molecular docking was conducted at the beginning of this study. The compounds were then synthesized from benzoyl chloride derivatives and N-phenylthiourea. Molecular structure was confirmed using FTIR, 1H NMR, 13C NMR and Mass Spectra, while the anticancer activity was tested in vitro against human breast cancer cells (T47D) using MTT assay. The results indicated that the anti-cancer activities of the test compounds were better than those of the hydroxyurea as the reference compound, evidenced by the Rerank Score (RS). Furthermore, cytotoxic effect of 3-Cl-BPTU (IC50: 0.43 mM) and 3,4-dichloro-BPTU (IC50: 0.85 mM) showed better result compared with hydroxyurea (IC50: 4.58 mM). Therefore, we concluded that these compounds could possess termendous potential as the candidate for a new anticancer drug.

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