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
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.
Papaconstantinou, Ioanna C.,Fousteris, Manolis A.,Koutsourea, Anna I.,Pairas, Georgios N.,Papageorgiou, Athanasios D.,Nikolaropoulos, Sotiris S.
p. 52 - 65
(2013/02/25)
Direct amino acid-catalyzed cascade reductive alkylation of arylacetonitriles: High-yielding synthesis of ibuprofen analogs
A novel approach for a one-pot, three-component reductive alkylation (TCRA) reaction of arylacetonitriles-containing electron-withdrawing groups with aldehydes/ketones and 1,4-dihydropyridine via iminium-catalysis has been developed. Many TCRA reaction products have direct applications in agricultural and pharmaceutical chemistry.
Ramachary, Dhevalapally B.,Shiva Prasad
scheme or table
p. 5246 - 5251
(2010/11/03)
SULFONAMIDE DERIVATIVES
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.
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(2008/06/13)
OXIDANT SENSITIVE AND INSENSITIVE AROMATIC ESTERS AS INHIBITORS OF HUMAN NEUTROPHIL ELASTASE
2-Phenylalkanoate esters which are useful as inhibitors of human leukocyte elastase.
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(2008/06/13)
Glutamine derivatives
Glutamine derivatives and non-toxic salts thereof have been found to have immunomodulating activities.
N-(1,3-dithiolan-2-ylidene)-4-alkylanilines having a hydroxy, alkoxy or alkanoyloxy substituent on the alkyl group are useful as anti-inflammatory agents, as analgesic agents and as antiasthmatic agents. The compounds involved can be prepared by the reaction of an appropriate 4-alkylaniline with a methyl(1,3-dithiolan-2-ylidene)sulfonium salt or with carbon disulfide and ethylene dibromide in the presence of a base.
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(2008/06/13)
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