Synthesis and cytotoxic activity of 17-carboxylic acid modified 23-hydroxy betulinic acid ester derivatives.
New 17-carboxylic acid modified 23-hydroxy betulinic acid ester derivatives were prepared and tested for cytotoxic activity on five cancer cell lines in vitro: all tested compounds showed stronger cytotoxic activity than 23-hydroxy betulinic acid and betulinic acid. In addition, compound 5a was tested for anti-tumor activity in vivo: it had much better anti-tumor activity than 23-OH betulinic acid and had similar anti-tumor activity with cyclophosphamide and 5-fluorouracil.
Bi
Yi
Y
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Xu
Jinyi
J
Wu
Xiaoming
X
Ye
Wencai
W
Yuan
Shengtao
S
Zhang
Luyong
L
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002264:Carboxylic Acids; D045744:Cell Line, Tumor; D004952:Esters; D006801:Humans; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy; D053978:Pentacyclic Triterpenes; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis* / Q000494:pharmacology; D047368:Tumor Burden / Q000187:drug effects; D000094062:Betulinic Acid
D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D004952:Esters; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid