Human polymorphonuclear neutrophils rapidly incorporated radiolabeled platelet-activating factor, 1-O-Ihexadecyl-9, 10-3H21-2-acetyl-sn-glycero-3-phosphocholine (I3HIPAF), and then metabolized it into its sn-2-fatty acyl derivative.
Combinations of an amidoalkylphosphocholine, 8, and AZT have been found to cause an apparent synergistic action in suppressing infectious HIV-1 replication. In addition, amidoalkyl, oxyalkyl, and thioalkyl ether lipids have been chemically linked to anti-HIV-1 nucleosides (AZT and DDI) through phosphate and phosphonate linkages. These conjugates have shown promising in vitro anti-HIV-1 activity. Also, the conjugates have a 5-10-fold reduction in cell cytotoxicity compared to AZT alone. The most active compound, an amidoalkyl ether lipid-AZT conjugates, 4A, was found to have a differential selectivity of 1793 in a syncytial plaque assay. In comparison, AZT alone has a value of 1281.
SynopsisSix vinyl phosphonates have been synthesized and evaluated as grafts on poly(ethy1ene terephthalate) for their flame retardance properties. Diethylvinyl phosphonate was used as a model for phosphorus-containing flame retardants in developing the methodology for localizing flame retardants either on the surface of the filament or uniformly throughout it. SEM-X-ray microprobe techniques were used in the verification of the location of the flame retardant in the filament. The flame retardance efficiency of poly(diethy1 vinyl phosphonate) was then correlated with its location in the filament. Other grafted phosphorus-containing flame retardants showed a range of efficiencies that depended not only upon the location of the graft within the filament but also upon the %P in the compound. The wide variations in flame retardance efficiencies of copolymers and terpolymers were attributed to large variations in the melt viscosity of the different grafted materials. The grafts showed only small changes in tenacity and large increases in elongation.
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.
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