Synthesis and evaluation of a DHA and 10-hydroxycamptothecin conjugate.
We have synthesized a conjugate of cis-4,7,10,13,16,19-docosahexenoic acid (DHA) and 10-hydroxycamptothecin (HCPT), DHA-HCPT. The antitumor activity of DHA-HCPT was evaluated in vitro against L1210 leukemia cells and in experimental animal tumor models including L1210 leukemia, Lewis lung carcinoma, and colon 38 adenocarcinoma. DHA-HCPT showed a greatly improved antitumor efficacy compared to HCPT.
Wang
Yuqiang
Y
Institute of New Drug Research, Jinan University College of Pharmacy, Guangzhou 510632, China. yuqiangwang2001@yahoo.com
Li
Lianfa
L
Jiang
Wei
W
Larrick
James W
JW
D000230:Adenocarcinoma / Q000188:drug therapy*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy*; D004195:Disease Models, Animal; D004281:Docosahexaenoic Acids / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy*; D051379:Mice; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; C506451:DHA-HCPT conjugate; D004281:Docosahexaenoic Acids; C028098:10-hydroxycamptothecin; D002166:Camptothecin