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,...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2005-10, Vol.13 (19), p.5592-5599
Main Authors: Wang, Yuqiang, Li, Lianfa, Jiang, Wei, Larrick, James W.
Format: Article
Language:English
Subjects:
Adenocarcinoma - drug therapy
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Biological and medical sciences
Camptothecin - analogs & derivatives
Camptothecin - chemical synthesis
Camptothecin - pharmacology
Carcinoma, Lewis Lung - drug therapy
Cell Line, Tumor
Cell Proliferation - drug effects
Colonic Neoplasms - drug therapy
Disease Models, Animal
Docosahexaenoic Acids - chemical synthesis
Docosahexaenoic Acids - pharmacology
Drug Design
Drug Screening Assays, Antitumor
General aspects
Humans
Leukemia L1210 - drug therapy
Medical sciences
Mice
Molecular Conformation
Pharmacology. Drug treatments
Stereoisomerism
Structure-Activity Relationship
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Summary: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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2005.06.039