103304-67-2Relevant academic research and scientific papers
Synthesis and biological activity of novel quaternary ammonium derivatives of alkylglycerols and potent inhibitors of protein kinase C
Marasco Jr.,Piantadosi,Meyer,Morris-Natschke,Ishaq,Small,Daniel
, p. 985 - 992 (2007/10/02)
Alyklglycerols such as rac-1-O-octadecyl-2-O-methylglycerophosphochocholine (Et-18-OMe) have shown an inhibitory effect on the metastasis and growth of various cancer cell lines. Alkyl phospholipids have been shown to accumulate at the surface in several cell lines, the selectivity of which is still not clearly understood. A consequence of this action may lead to the inhibition of cell membrane related protein kinase C (PKC). The goal of this research was to develop ether lipid inhibitors of PKC to augment antineoplastic activity. This led to the synthesis and in vitro testing of a series of novel quaternary ammonium derivatives of alkylglycerols. The biological testing of these analogues on PKC stimulated with rac-1-O-oleoyl-2-O-acetylglycerol showed several analogues with inhibition comparable to that of Et-18-OMe.
Synthesis of Sulfur Analogues of Alkyl Lysophospholipid and Neoplastic Cell Growth Inhibitory Properties
Morris-Natschke, Susan,Surles, Jefferson R.,Daniel, Larry W.,Berens, Michael E.,Modest, Edward J.,Piantadosi, Claude
, p. 2114 - 2117 (2007/10/02)
Five sulfur-containing phospholipid analogues (compounds 1-5) of alkyl lysophospholipid (1-O-alkyl-2-O-methyl-rac-glycero-3-phosphocholine, ALP) were synthesized and tested for inhibition of neoplastic cell proliferation with two human ovarian carcinoma cell lines in a clonogenic assay and with the HL-60 promyelocytic leukemia cell line.Compared with 1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine (ET-18-OMe), the most active reference analogue, these thio analogues are at least as active against HL-60 cells, and the 1-S-hexadecyl-2-O-ethyl analogue (2) is twice as active in the clonogenic assays.
