Synthesis and evaluation of new 3-substituted-4-chloro-thioxanthone derivatives as potent anti-breast cancer agents

Chun Liang Chen, Tsung Chih Chen, Chia Chung Lee, Liu Chuan Shih, Chih Yuan Lin, Ying Yu Hsieh, Ahmed Atef Ahmed Ali, Hsu Shan Huang

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

A series of 3-substituted-4-chloro-thioxanthones and their corresponding S,S-dioxidethioxanthone derivatives were designed and synthesized. The effects of our synthesized compounds on cell viability toward the MCF-7 and MDA-MB-468 breast cancer cell lines were evaluated. The most active compound was 4f, which was active against the MCF-7 and MDA-MB-468 cell lines with respective IC50 values of 7.2 and 3.9μM. Interestingly, compound 4f did not impair cell viability of the cardiac myoblast H9C2 cell line (IC50 >25μM), indicating that this compound might not exhibit cytotoxic effects on the normal cardiac cells. Further, compounds 4b, 4f, 4j, 4s, 5b, 5f, 5j, and 5s were characterized by the NCI screening system. Results revealed that compounds 4f and 4s had effective anticancer activities against various cancer cell lines. Finally, our results indicated that the 3-substituted-4-chloro-thioxanthone derivatives have the potential to be further developed as promising small molecules for anticancer applications.

Original languageEnglish
JournalArabian Journal of Chemistry
DOIs
Publication statusPublished - 2015

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Cells
Derivatives
thioxanthone
Screening
Molecules

Keywords

  • MCF-7
  • MDA-MB-468
  • NCI 60-cell panel assay
  • Thioxanthen-9-one-10,10-dioxide
  • Thioxanthone

ASJC Scopus subject areas

  • Chemical Engineering(all)
  • Chemistry(all)

Cite this

Synthesis and evaluation of new 3-substituted-4-chloro-thioxanthone derivatives as potent anti-breast cancer agents. / Chen, Chun Liang; Chen, Tsung Chih; Lee, Chia Chung; Shih, Liu Chuan; Lin, Chih Yuan; Hsieh, Ying Yu; Ali, Ahmed Atef Ahmed; Huang, Hsu Shan.

In: Arabian Journal of Chemistry, 2015.

Research output: Contribution to journalArticle

Chen, Chun Liang ; Chen, Tsung Chih ; Lee, Chia Chung ; Shih, Liu Chuan ; Lin, Chih Yuan ; Hsieh, Ying Yu ; Ali, Ahmed Atef Ahmed ; Huang, Hsu Shan. / Synthesis and evaluation of new 3-substituted-4-chloro-thioxanthone derivatives as potent anti-breast cancer agents. In: Arabian Journal of Chemistry. 2015.
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abstract = "A series of 3-substituted-4-chloro-thioxanthones and their corresponding S,S-dioxidethioxanthone derivatives were designed and synthesized. The effects of our synthesized compounds on cell viability toward the MCF-7 and MDA-MB-468 breast cancer cell lines were evaluated. The most active compound was 4f, which was active against the MCF-7 and MDA-MB-468 cell lines with respective IC50 values of 7.2 and 3.9μM. Interestingly, compound 4f did not impair cell viability of the cardiac myoblast H9C2 cell line (IC50 >25μM), indicating that this compound might not exhibit cytotoxic effects on the normal cardiac cells. Further, compounds 4b, 4f, 4j, 4s, 5b, 5f, 5j, and 5s were characterized by the NCI screening system. Results revealed that compounds 4f and 4s had effective anticancer activities against various cancer cell lines. Finally, our results indicated that the 3-substituted-4-chloro-thioxanthone derivatives have the potential to be further developed as promising small molecules for anticancer applications.",
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AU - Lin, Chih Yuan

AU - Hsieh, Ying Yu

AU - Ali, Ahmed Atef Ahmed

AU - Huang, Hsu Shan

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