Steroidal esters of the aromatic nitrogen mustard 2-[4-N, N-bis (2-chloroethyl) amino-phenyl] butanoic acid (2-PHE-BU): synthesis and in-vivo biological evaluation

…, AI Koutsourea, GN Pairas, AD Papageorgiou…

Index: Papaconstantinou, Ioanna C.; Fousteris, Manolis A.; Koutsourea, Anna I.; Pairas, Georgios N.; Papageorgiou, Athanasios D.; Nikolaropoulos, Sotiris S. Anti-Cancer Drugs, 2013 , vol. 24, # 1 p. 52 - 65

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Abstract

Abstract On the basis of the results of in-silico predictions and in an effort to extend our structure–activity relationship studies, the aromatic nitrogen mustard 2-[4-N, N-bis (2- chloroethyl) amino-phenyl] butanoic acid (2-PHE-BU) was synthesized and conjugated with various steroidal alcohols. The resulting steroidal esters were evaluated for their in-vivo toxicity and antileukemic activity in P388-leukemia-bearing mice. The new derivatives ...

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