Sombut Sudarat, Bunthawong Rada, Sirion Uthaiwan, Kasemsuk Teerapich, Piyachaturawat Pawinee, Suksen Kanoknetr, Suksamrarn Apichart, Saeeng Rungnapha
Department of Chemistry and Center for Innovation in Chemistry, Faculty of Science, Burapha University, Chonburi 20131, Thailand.
Department of Chemistry, Faculty of Science and Technology, Rambhai Barni Rajabhat University, Chanthaburi 22000, Thailand.
Bioorg Med Chem Lett. 2017 Dec 1;27(23):5139-5143. doi: 10.1016/j.bmcl.2017.10.063. Epub 2017 Oct 30.
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 EDs 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.
以天然存在的穿心莲内酯为原料合成了一系列14-脱氧-11,12-二脱氢穿心莲内酯类似物，并评估了它们对包括胆管癌在内的9种癌细胞系的细胞毒性。类似物5a和5b表现出最强的细胞毒性，对KKU-M213细胞系的半数有效剂量（ED）分别为3.37和3.08 μM，对KKU-100细胞系的ED分别为2.93和3.27 μM。本研究中确定的对胆管癌细胞系的选择性细胞毒性突出了结构修饰在该癌症药物开发中的重要性。
