945226-22-2Relevant articles and documents
Annonaceous acetogenin mimics bearing a terminal lactam and their cytotoxicity against cancer cells
Liu, Hai-Xia,Huang, Guo-Rui,Zhang, Huan-Ming,Wu, Jia-Rui,Yao, Zhu-Jun
, p. 3426 - 3430 (2008/02/09)
Annonaceous acetogenins are a large class of naturally occurring polyketides exhibiting potent anticancer activities. Based on our previous discovery of AA005, a multi-ether mimic of natural acetogenins having potent antitumor activities and significant selectivity between normal cells and cancer cells, a new series of mimics containing a terminal lactam were designed, synthesized and evaluated. Bioactivity study against cancer cells shows that the N-methylated lactam-containing compounds 3, 4, and 5 exhibit comparable potencies to that of AA005, as well as the similar selectivity to cancer cells. Hydrocarbon-length effects of N-alkyl were further explored through synthesizing derivatives 24-26, and application of this derivation protocol to the fluorescent labeling was also investigated.
