46406-87-5Relevant articles and documents
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.
SULFONAMIDE DERIVATIVES
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, (2008/06/13)
A sulfonamide derivatives of formula (I) STR1 a non-toxic salts, an acid addition salts or a solvates thereof which has an inhibitory effect on elastase.
Glutamine derivatives
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, (2008/06/13)
Glutamine derivatives and non-toxic salts thereof have been found to have immunomodulating activities.
