151391-75-2Relevant academic research and scientific papers
Design and synthesis of heterobimetallic topoisomerase I and II inhibitor complexes: In vitro DNA binding, interaction with 5′-GMP and 5′-TMP and cleavage studies
Arjmand, Farukh,Muddassir, Mohd.
, p. 37 - 46 (2010)
New potential cancer chemotherapeutic complexes Cu-Sn2/Zn-Sn2 3 and 4 were designed and prepared as topoisomerases inhibitors; their in vitro DNA binding studies were carried out which reveal strong electrostatic binding via phosphat
Late metal salicylaldimine complexes derived from 5-aminosalicylic acid - Molecular structure of a zwitterionic mono Schiff base zinc complex
Bourque, Tara A.,Nelles, Megan E.,Gullon, Teri J.,Garon, Christian N.,Ringer, Melissa K.,Leger, Lisa J.,Mason, Jamie W.,Wheaton, Susan L.,Baerlocher, Felix J.,Vogels, Christopher M.,Decken, Andreas,Westcott, Stephen A.
, p. 1063 - 1070 (2007/10/03)
Condensation of salicylaldehyde (2-HOC6H4C(O)H) with 5-aminosalicylic acid (5-H2NC6H3-2-(OH)-CO 2H) afforded the Schiff base 2-HOC6H4C(H)= NC6H3-
Effect of 5-substituted benzylideneaminosalicylic acid on carrageenan-induced ulcerative colitis.
Jaysekhar,Rao,Santhakumari
, p. 309 - 313 (2007/10/03)
Mesalazine, a drug of choice in the management of ulcerative colitis, was chemically modified as 5-(E)-substituted benzylideneaminosalicylic acid by condensing 5-aminosalicylic acid with selected aryl aldehydes with an intention to improve its pharmacological profile. The tests were performed to study their anti-inflammatory effect on carrageenan-induced ulcerative colitis in albino rats. The histopathological findings, serum transaminase level and lipid peroxide content in the intestine and liver were taken as indices of pharmacological activity. The azomethine derivative formed from salicylaldehyde (5-ASASB3) was found to have maximum activity and it reversed the disease symptoms in experimental animals The azomethine derivative markedly reduces the ulcerative colitis when compared with parent molecule, mesalazine.
Synthesis and Structure-Activity Studies of a Series of salicylates as Inhibitors of EGF Receptor-Associated Tyrosine Kinase Activity
Chen, Huixiong,Boiziau, Janine,Parker, Fabienne,Maroun, Rachid,Tocque, Bruno,et al.
, p. 4094 - 4098 (2007/10/02)
The synthesis and structure-activity relationships of a series of salicylates and a series of salicylates as inhibitors of EGF receptor-associated tyrosine kinase activity are described.Their inhibitory potency was evaluated in vitro using ER 22 cell membranes (CCL 39 cells transfected with EGF receptor) as an enzyme source and the tridecapeptide RRSrc (RRLIEDAEYAARG) as substrate.Their cellular activity was measured by inhibition of the EGF-stimulated DNA synthesis of ER 22 cells.Chemical modifications were made to analyze the role of the different substituents.The amino series was found to be more active than the imino series.The hydroquinone moiety appears to be essential for tyrosine kinase inhibitory activity in the series of 5-salicylates.Comparison of the imino and amino series by molecular modeling techniques provides further evidence in support of the hypothesis that the important reduced linking chain, CH2NH allows the correct positioning of the 2,5-dihydroxybenzyl ring, possibly in a cis-like conformational arrangement.
