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Short Paper | Regular issue | Vol 98, No. 7, 2019, pp.977-983
Published online, 9th July, 2019
DOI: 10.3987/COM-19-14108
Semisynthesis of Triptolide Analogues Part IV: Effects of C-14 Carbamothioate Substituents on Cytotoxic Activities

Yutaka Aoyagi,* Mizuki Murase, Chihiro Kuwahara, Reiko Yano, Ritsuo Aiyama, Takeshi Matsuzaki, Shusuke Hashimoto, Haruhiko Fukaya, Koichi Takeya, and Yukio Hitotsuyanagi*

*College of Pharmacy, Kinjo Gakuin University, 2-1723 Omori, Moriyama-ku, Nagoya 463-8521, Japan


Four C-14 carbamothioate triptolide analogues were prepared and their cytotoxic activities on A549 human lung tumor cells and HT29 human colon tumor cells were evaluated. The activities of the prepared compounds were weaker than those of the parent compound, triptolide (1). However, some differences were noted in the activities of prepared compounds. The leaving ability and bulkiness of the amine components of their carbamothioate groups appeared to affect their cytotoxic activities.