2. Academic Validation
  3. Synthesis of 14-deoxy-11,12-didehydroandrographolide analogues as potential cytotoxic agents for cholangiocarcinoma

Synthesis of 14-deoxy-11,12-didehydroandrographolide analogues as potential cytotoxic agents for cholangiocarcinoma

  • Bioorg Med Chem Lett. 2017 Dec 1;27(23):5139-5143. doi: 10.1016/j.bmcl.2017.10.063.
Sudarat Sombut 1,  Rada Bunthawong 1,  Uthaiwan Sirion 1,  Teerapich Kasemsuk 2,  Pawinee Piyachaturawat 3,  Kanoknetr Suksen 3,  Apichart Suksamrarn 4,  Rungnapha Saeeng 5
Affiliations

Affiliations

  • 1 Department of Chemistry and Center for Innovation in Chemistry, Faculty of Science, Burapha University, Chonburi 20131, Thailand.
  • 2 Department of Chemistry, Faculty of Science and Technology, Rambhai Barni Rajabhat University, Chanthaburi 22000, Thailand.
  • 3 Department of Physiology, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
  • 4 Department of Chemistry, Faculty of Science, Ramkhamhaeng University, Bangkok 10240, Thailand.
  • 5 Department of Chemistry and Center for Innovation in Chemistry, Faculty of Science, Burapha University, Chonburi 20131, Thailand. Electronic address: rungnaph@buu.ac.th.
PMID: 29097170 DOI: 10.1016/j.bmcl.2017.10.063
Abstract

A series of 14-deoxy-11,12-didehydroandrographolide analogues were synthesized from naturally occurring andrographolide and their cytotoxicity evaluated against nine Cancer cell lines including cholangiocarcinoma. Analogues 5a and 5b exhibited the most potent cytotoxicity with ED50s of 3.37 and 3.08 μM on KKU-M213 cell lines and 2.93 and 3.27 μM on KKU-100 cell lines, respectively. Selective cytotoxicity on cholangiocarcinoma cell lines identified in this study highlight the importance of structural modification in the development of drugs for this Cancer.

Keywords

12-didehydroandrographolide; 14-Deoxy-11; Andrographis paniculata Nees; Cholangiocarcinoma; Cytotoxic activity.

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