Racemic l-O-(2-methyloctadecyl)-2-O-acetyl-glycero-3-phosphocholine, a branched chain PAF species, was prepared by chemical synthesis and investigated for biological activity on human blood platelets in vitro. The synthesis started from 2-O-benzylglycerol and 2-methyloctadecyl-l-methyl sulfonate and
Tritium Labelled 1-O-Octadecyl-2-O-methyl-rac-glycero-3-phosphocholine (ALP) and 1-S-Hexadecyl-2-O-ethyl-rac-thioglycero-3-phosphocholine (Thio-ALP)
โ Scribed by Steven D. Wyrick; Jefferson R. Surles; Susan Morris-Natschke; Claude Piantadosi; Edward J. Modest
- Publisher
- John Wiley and Sons
- Year
- 1989
- Tongue
- French
- Weight
- 288 KB
- Volume
- 27
- Category
- Article
- ISSN
- 0022-2135
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โฆ Synopsis
The phospholipids, ALP and Thio-ALP, are non-hydrolyzable analogues of platelet activating factor (PAF).
Interest i n ALP and thio-ALP centers upon their activity as potential antineoplastic agents. A variety of mechanisms of action have been attributed to these compounds including inhibiti$q of a phospholipid cofactor of a phospholipid sensitive Ca -dependent protein kinase. Thio-ALP is at least as active as a growth inhibitor of the HL-60 promyelocytic leukemic cell line as is ALP-the most active reference analogue reported in the literature and is approximately twice as active against the BG-1 and BG-3 human ovarian carcinoma cell lines. To aid in further biochemical studies, we report the synthesis of high specific activity tritium labelled ALP and thio-ALP. These products were obtained by palladium catalyzed reduction of 1-0-octadecenyl and 1-S-hexadecenyl precursors with carrier-free tritium gas.
๐ SIMILAR VOLUMES
Boron-containing analogues of ether lipids are proposed as boron carriers in the boron neutron capture therapy (BNCT). The syn-the~ of rac-I-(9-o-Carboranyl)nonyl-2-methyl-glycero-3-phosphocholine (B-Et-I l-OMe) as a in'st representative is described. The carborane is introduced into the readily ass