Synthesis and antitumor activity of 20-O-linked nitrogen-based camptothecin ester derivatives.
A series of nitrogen-based 20S-hydroxyl camptothecin ester derivatives were prepared. 3-Aminopropionate of camptothecin was found more cytotoxic in vitro on several human tumor cell lines than 3-amidopropionate of camptothecin. Ester 16 showed best antitumor activity in vivo and in vitro in all esters we prepared.
Wang
Cun-ying
CY
School of Chemical Engineering and Technology, China University of Mining and Technology, Xuzhou 221008, China.
Pan
Xian-dao
XD
Liu
Hong-yan
HY
Fu
Zhao-di
ZD
Wei
Xian-yong
XY
Yang
Li-Xi
LX
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D002166:Camptothecin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D004952:Esters / Q000737:chemistry*; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology; D015394:Molecular Structure; D009584:Nitrogen / Q000737:chemistry*; D023041:Xenograft Model Antitumor Assays
D000970:Antineoplastic Agents; D004952:Esters; D009584:Nitrogen; D002166:Camptothecin