Antitumor activity of a piperidine phospholipid.

Abstract	A piperidine phospholipid ((+/-)-2-[hydroxy] [1-octadecyloxycarbonylpiperidin-3-yl]methoxy-phosphinyl] oxy]-N,N,N, trimethylethaniminium hydroxide inner salt, SDZ 62-826) has been prepared that exhibited weak direct cytotoxicity and strong macrophage-induced cytotoxicity in vitro against a variety of murine and one human tumor cell lines. This compound was found to be as effective as ET-18-OCH3 and SRI 62-834, phospholipids with both strong direct and macrophage-induced cytotoxicity, in increasing survivors and reducing tumor volume when given either orally or intravenously in the mouse MethA fibrosarcoma model. These findings suggest that the macrophage-induced cytotoxicity exhibited by ET-18-OCH3 and other phospholipids may play an important role in this tumor model.
Authors	W J Houlihan, M L Lee, P G Munder, D A Handley, G A Nemecek, C S Jaeggi, C W Winslow
Journal	Arzneimittel-Forschung (Arzneimittelforschung) Vol. 44 Issue 12 Pg. 1384-8 (Dec 1994) ISSN: 0004-4172 [Print] Germany
PMID	7848363 (Publication Type: Journal Article)
Chemical References	Antineoplastic Agents Phospholipid Ethers Piperidines Platelet Activating Factor Platelet Aggregation Inhibitors Platelet Membrane Glycoproteins Receptors, Cell Surface Receptors, G-Protein-Coupled SDZ 62-826 platelet activating factor receptor Receptors, Platelet-Derived Growth Factor
Topics	Animals Antineoplastic Agents (chemical synthesis, pharmacology, therapeutic use) Binding, Competitive (drug effects) Cell Survival (drug effects) Fibroblasts (drug effects) Fibrosarcoma (drug therapy) Humans Lethal Dose 50 Macrophages (drug effects) Mice Mice, Inbred BALB C Mice, Inbred C57BL Neoplasm Transplantation Phospholipid Ethers (chemical synthesis, pharmacology, therapeutic use) Piperidines (chemical synthesis, pharmacology, therapeutic use) Platelet Activating Factor (metabolism) Platelet Aggregation Inhibitors (pharmacology) Platelet Membrane Glycoproteins (drug effects) Receptors, Cell Surface Receptors, G-Protein-Coupled Receptors, Platelet-Derived Growth Factor (drug effects) Sarcoma, Experimental (drug therapy) Tumor Cells, Cultured

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