Heterocyclic 1,2-epoxyalkan-3-ones as cytotoxic agents
A series of 1->-1,2-epoxybutan-3-ones 13 and 1--1,2-epoxyalkan-3-ones 12, 16 and 17 was synthesized.In vitro screening against L1210 leukemic cells indicated that the stereochemistry of the oxiranyl sustituents and/or size of the R2 alkyl substituents are determinants of cytotoxic activity.Increasing the length of the R2 alkyl substituent for trans-16 decreased activity.The lipophilic effect of the R2 substituent does not appear to be a significant determinant of activity.Some structure-activity correlations are described.Keywords - cytotoxic agents / pyridines / 1,2-epoxyalkan-3-ones.
Vo, Dean,Agarwal, Kamlesh C.,Knaus, Edward E.,Allen Theresa M.,Fathi-Afshar, R.
p. 39 - 44
(2007/10/02)
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