Influence of 1-beta-D-arabinofuranosylcytosine conjugates of lipids on the growth and metastasis of Lewis lung carcinoma.

Abstract

Five different lipid conjugates of 1-beta-D-arabinofuranosylcytosine (ara-C) were tested for their therapeutic activity on the growth and metastasis of Lewis lung carcinoma (3-LL). Among 1 ester-linked lipid conjugate (Ara-CDP-L-dipalmitin), 3 1-O-alkyl-lipid conjugates (ara-CDP-D,L-PBA, ara-CDP-D,L-PCA, ara-CDP-D,L-MBA) and a thioether-lipid conjugate (ara-CDP-D,L-PTBA) ara-CDP-D,L-PTBA, ara-CDP-D,L-PBA, and ara-CDP-L-dipalmitin produced the strongest tumor growth inhibition and increase of surviving animals in C57Bl6-mice bearing i.p.-implanted 3-LL. Furthermore these conjugates were superior to the parent compounds alone, or equimolar mixtures of the alkyllysophospholipid derivatives ET-18-OCH3 and ara-C. Successful therapeutic regimen consisted of 80-100 mg conjugate/kg, given i.p. daily for five consecutive days. Similar regimen injected shortly after the surgical removal of the primary tumor as adjuvant chemotherapy inhibited the metastasis of 3-LL to the lungs of the animals as demonstrated by an increase of survival time and the number of surviving animals.

• Authors: W E Berdel, S Danhauser, C I Hong, H D Schick, A Reichert, R Busch, J Rastetter, W R Vogler
• Journal: Cancer research (Cancer Res) Vol. 48 Issue 4 Pg. 826-9 (Feb 15 1988) ISSN: 0008-5472 [Print] United States
• PMID: 3338080 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Esters
• Lipids
• Cytarabine

Topics

• Animals
• Cytarabine (analogs & derivatives, therapeutic use)
• Esters
• Female
• Lipids (therapeutic use)
• Lung Neoplasms (drug therapy, pathology, secondary)
• Mice
• Mice, Inbred C57BL
• Neoplasm Metastasis
• Structure-Activity Relationship