Synthesis and biological evaluation of gemcitabine–lipid conjugate (NEO6002)

The synthesis and biological evaluation of novel gemcitabine–lipid conjugate is reported. A novel gemcitabine–lipid conjugate 5 was synthesized and tested for its in vivo efficacy and toxicity. Compound 5 was tested in BxPC-3 human pancreatic tumor model in SCID mice and exhibited promising activity...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-05, Vol.15 (10), p.2571-2574
Main Authors: Ali, Shoukath M., Khan, Abdul R., Ahmad, Moghis U., Chen, Paul, Sheikh, Saifuddin, Ahmad, Imran
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cardiolipin
Cell Line, Tumor
Deoxycytidine - analogs & derivatives
Deoxycytidine - chemical synthesis
Deoxycytidine - pharmacology
Drug Screening Assays, Antitumor
Gemcitabine
General aspects
Humans
Lipids - chemical synthesis
Lipids - pharmacology
Lipid–nucleoside conjugate
Medical sciences
Mice
Mice, SCID
Pharmacology. Drug treatments
Prodrug
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Summary:The synthesis and biological evaluation of novel gemcitabine–lipid conjugate is reported. A novel gemcitabine–lipid conjugate 5 was synthesized and tested for its in vivo efficacy and toxicity. Compound 5 was tested in BxPC-3 human pancreatic tumor model in SCID mice and exhibited promising activity and lower toxicity when compared with Gemzar®.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.03.046