57960-84-6Relevant academic research and scientific papers
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
Papaconstantinou, Ioanna C.,Fousteris, Manolis A.,Koutsourea, Anna I.,Pairas, Georgios N.,Papageorgiou, Athanasios D.,Nikolaropoulos, Sotiris S.
, p. 52 - 65 (2013/02/25)
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 showed significantly reduced toxicity and marginally improved antileukemic activity compared with free 2-PHE-BU. Nevertheless, they did not prove to be superior either to the template steroidal ester used for in-silico predictions or to previously synthesized steroidal esters of aromatic nitrogen mustards. The results obtained indicate that in-silico design predictions may guide the design and synthesis of new bioactive steroidal esters, but further parameters should be considered aiming at the discovery of compounds with optimum activity.
Glutamine derivatives
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, (2008/06/13)
Glutamine derivatives and non-toxic salts thereof have been found to have immunomodulating activities.
Tertiary aminoacids
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, (2008/06/13)
New α-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula STR1 and functional derivatives thereof, are anti-inflammatory agents.
Tertiary aminoacids
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, (2008/06/13)
New α-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula STR1 AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.
