Dymond, M.K. and Attard, G.S.
Structure-activity relationships in anti-neoplastic: type I amphiphiles
Biochemistry, 39, (6), . (doi:10.1021/bi9950995).
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HDPC and ET-18-OMe, both type I amphiphiles and analogues of the naturally occurring biomembrane component lysophosphatidylcholine, are potent anti-neoplastic agents. A series of novel, type I amphiphiles have been synthesized, and their cytostatic activity against cancer cells in culture was determined. The data suggest that cytostatic activity is a generic property of type I amphiphiles. Furthermore, the primary target for these amphiphiles appears to be the inhibition of phosphatidylcholine synthesis via perturbation in the elastic properties of intracellular bilayer membranes.
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