Synthesis and anticancer evaluation of N-benzoyl-N'-phenyltiourea derivatives against human breast cancer cells (T47D)

doi:10.5246/jcps.2020.02.010

中国药学(英文版) ›› 2020, Vol. 29 ›› Issue (2): 123-129.DOI: 10.5246/jcps.2020.02.010

Synthesis and anticancer evaluation of N-benzoyl-N'-phenyltiourea derivatives against human breast cancer cells (T47D)

Dini Kesuma¹, Siswandono², Bambang Tri Purwanto^2*, Marcellino Rudyanto²

1. Faculty of Pharmacy, Surabaya University, Surabaya, Indonesia
2. Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia

收稿日期:2019-10-16 修回日期:2019-12-11 出版日期:2020-02-29 发布日期:2019-12-17
通讯作者: Tel.: +62-8123536513, E-mail: bambangsutony@gmail.com
基金资助:
Directorate General of Resources for Science, Technology and Higher Education of Ministry of Research, Technology and Higher Education (Kemristek Dikti) with scheme of scholarship funding for Phd program at University of Airlangga.

Synthesis and anticancer evaluation of N-benzoyl-N'-phenyltiourea derivatives against human breast cancer cells (T47D)

Dini Kesuma¹, Siswandono², Bambang Tri Purwanto^2*, Marcellino Rudyanto²

1. Faculty of Pharmacy, Surabaya University, Surabaya, Indonesia
2. Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia

Received:2019-10-16 Revised:2019-12-11 Online:2020-02-29 Published:2019-12-17
Contact: Tel.: +62-8123536513, E-mail: bambangsutony@gmail.com
Supported by:
Directorate General of Resources for Science, Technology and Higher Education of Ministry of Research, Technology and Higher Education (Kemristek Dikti) with scheme of scholarship funding for Phd program at University of Airlangga.

摘要/Abstract

摘要：

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.

关键词: N-(3-chloro)benzoyl-N'-phenylthiourea, N-(3,4-dichloro)benzoyl-N'-phenylthiourea, Anticancer, T47D cells, SIRT1

Abstract:

Key words: N-(3-chloro)benzoyl-N'-phenylthiourea, N-(3,4-dichloro)benzoyl-N'-phenylthiourea, Anticancer, T47D cells, SIRT1

中图分类号:

R914

Supporting:

Dini Kesuma, Siswandono, Bambang Tri Purwanto, Marcellino Rudyanto. Synthesis and anticancer evaluation of N-benzoyl-N'-phenyltiourea derivatives against human breast cancer cells (T47D)[J]. 中国药学(英文版), 2020, 29(2): 123-129.

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Synthesis and anticancer evaluation of N-benzoyl-N'-phenyltiourea derivatives against human breast cancer cells (T47D)

Synthesis and anticancer evaluation of N-benzoyl-N'-phenyltiourea derivatives against human breast cancer cells (T47D)

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