13879-87-3Relevant articles and documents
Nucleoside Conjugates. 14. Synthesis and Antitumor Activity of 1-β-D-Arabinofuranosylcytosine Conjugates of Ether Lipids with Improved Water Solubility
Hong, Chung Il,Nechaev, Alexander,Kirisits, Alan J.,Vig, Rakesh,Hui, Sek-Wen,West, Charles R.
, p. 1629 - 1634 (1995)
A series of ara-CDP-rac-1-O-alkyl-2-O-acylglycerols (9a-f), analogues of highly active ara-CDP-rac-1-O-hexadecyl-2-O-palmitoylglycerol (1) and Cytoros (2), was prepared, and solubility, lipophilicity, and structure-activity relationships of these conjugates were investigated.Conjugates 9a-f containing sn-1 alkyl (C16) and the sn-2 fatty acyl (>C16) such as conjugate 1 were sparingly soluble.Conjugates 9a-c,e were almost completely solubilized in water by shaking.However, a large portion of conjugates 9d and 9f in water by shaking exist in micelles with mean diameters ranging 7.0-55.2 nm.The partition coefficients (1-octanol/PBS) of the water-soluble conjugates were about 9-18 times greater than that of ara-C.A single dose (300 mg/kg) of conjugates 9d and 9f produced a significant increase in life span (ILS 206 to >543percent) with 17-67percent long-term survivors (>45 days) in mice bearing ip-implanted L1210 lymphoid leukemia.These results were comparable to those of the previous conjugate 1 and Cytoros (2).In contrast,conjugates 9a-c,e at single doses were less effective (ILS 69-178percent with no long-term survivors).However, two (qd, 1, 7) or three (qd 1, 5, 9) divided doses of these conjugates were found to be as effective as a single dose of the previous conjugates.The three divided doses (150 mg/kg per day) of conjugates 9d, 9e, and 9f produced a remarkable antitumor activity in L1210 leukemic mice (ILS >350percent with >50percent long-term servivors).Because of the convenient formulation and the significant antitumor activities, the water-soluble conjugates 9d, 9e, and 9f warrant further investigation.
Synthesis of lipid-oligonucleotide conjugates for RNA interference studies
Grijalvo, Santiago,Ocampo, Sandra M.,Perales, Jose C.,Eritja, Ramon
experimental part, p. 287 - 299 (2011/10/03)
The synthesis of RNA molecules carrying lipids at their 3′-termini and 5′-termini is reported. These conjugates were fully characterized by MALDI-TOF mass spectrometry and HPLC chromatography. The ability of these conjugates to silence gene expression was
Compositions containing lysophosphatidic acids which inhibit apoptosis and uses thereof
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Page/Page column 36, (2008/06/13)
The invention provides anti-apoptotic compositions lysophosphatidic acids and methods for making and using the compositions. Such compositions can also contain LPA potentiating agents, including proteins, lipid membrane structures and polymers such as polyethylene glycols. The compositions can additionally contain other pharmaceutically effective agents such as drugs, antibiotics, wound healing agents and antioxidants.