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.

中文翻译：

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合成14-脱氧11,12-二氢脱水穿心莲内酯类似物作为胆管癌的潜在细胞毒剂

从天然存在的穿心莲内酯中合成了一系列的14-脱氧-11,12-二氢-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，在KKU-M213细胞系上ED _50分别为3.37和3.08μM，在KKU-100细胞系上为2.93和3.27μM。在这项研究中确定的胆管癌细胞系的选择性细胞毒性突显了结构修饰在该癌症药物开发中的重要性。