1430823-79-2Relevant academic research and scientific papers
Synthesis and structure-activity relationships study of cytotoxic bufalin 3-nitrogen-containing-ester derivatives
Ma, Biao,Xiao, Zhi-Yong,Chen, Yi-Jia,Lei, Min,Meng, Yu-Hui,Guo, De-An,Liu, Xuan,Hu, Li-Hong
, p. 508 - 512 (2013/06/26)
A series of bufalin 3-nitrogen-containing-ester derivatives (2-6) were designed, synthesized, and evaluated for their proliferation inhibition activities against human cervical epithelial adenocarcinoma (HeLa) and non-small-cell lung cancer (A549) cell lines. The structure-activity relationships (SARs) of this new series were described in this paper. Cytotoxicity data revealed that C3 moiety had important influence on cytotoxic activity. On two cell lines, the bufalin-3-piperidinyl-4-carboxylate compound 2 (IC50 values on HeLa and A549 cell lines were 0.76 nM and 0.34 nM, respectively) displayed a significant cytotoxic potency compared to the parent compound bufalin.
