Synthesis and cytotoxicity of 2-cyano-28-hydroxy-lup-1-en-3-ones.
New A-ring modified betulin and dihydrobetulin derivatives possessing the 2-cyano-1-en-3-one moiety were prepared and tested for cytotoxicity in seven cancer cell lines. The most active agent 9a synthesized in this account was further demonstrated to induce apoptosis and to activate caspases in malignant melanoma cells.
Koohang
Ali
A
Advanced Life Sciences, Inc, Research and Development, Woodridge, IL 60517, USA.
Majewski
Nathan D
ND
Szotek
Erika L
EL
Mar
Aye Aye
AA
Eiznhamer
David A
DA
Flavin
Michael T
MT
Xu
Ze-Qi
ZQ
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006131:Growth Inhibitors / Q000138:chemical synthesis* / Q000633:toxicity*; D006801:Humans; D053978:Pentacyclic Triterpenes; D014315:Triterpenes / Q000138:chemical synthesis* / Q000633:toxicity*; D000094062:Betulinic Acid
D000972:Antineoplastic Agents, Phytogenic; D006131:Growth Inhibitors; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid