63452-52-8Relevant academic research and scientific papers
Insights about resveratrol analogs against trypanothione reductase of Leishmania braziliensis: Molecular modeling, computational docking and in vitro antileishmanial studies
da Silva, Adilson D.,dos Santos, Juliana A.,Machado, Patrícia A.,Alves, Lara A.,Laque, Larissa C.,de Souza, Vinícius C.,Coimbra, Elaine S.,Capriles, Priscila V. S. Z.
, p. 2960 - 2969 (2019/01/04)
In this work, we combined molecular modeling, computational docking and in vitro analysis to explore the antileishmanial effect of some resveratrol analogs (ResAn), focusing on their pro-oxidant effect. The molecular target was the trypanothione reductase
Pyrrole ketone compound and its preparation method and application
-
Paragraph 0072; 0073, (2017/09/02)
The invention discloses pyrrolone compounds as well as a preparation method and application thereof, wherein the pyrrolone compounds comprise an enantiomer, a diastereoisomer, a raceme and a mixture thereof, as well as pharmaceutically acceptable salt and
2,4-dihydroxy benzaldehyde derived Schiff bases as small molecule Hsp90 inhibitors: Rational identification of a new anticancer lead
Dutta Gupta, Sayan,Revathi,Mazaira, Gisela I.,Galigniana, Mario D.,Subrahmanyam,Gowrishankar,Raghavendra
, p. 97 - 105 (2015/03/14)
Hsp90 is a molecular chaperone that heals diverse array of biomolecules ranging from multiple oncogenic proteins to the ones responsible for development of resistance to chemotherapeutic agents. Moreover they are over-expressed in cancer cells as a complex with co-chaperones and under-expressed in normal cells as a single free entity. Hence inhibitors of Hsp90 will be more effective and selective in destroying cancer cells with minimum chances of acquiring resistance to them. In continuation of our goal to rationally develop effective small molecule azomethines against Hsp90, we designed few more compounds belonging to the class of 2,4-dihydroxy benzaldehyde derived imines (1-13) with our validated docking protocol. The molecules exhibiting good docking score were synthesized and their structures were confirmed by IR, 1H NMR and mass spectral analysis. Subsequently, they were evaluated for their potential to suppress Hsp90 ATPase activity by Malachite green assay. The antiproliferative effect of the molecules were examined on PC3 prostate cancer cell lines by adopting 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay methodology. Finally, schiff base 13 emerged as the lead molecule for future design and development of Hsp90 inhibitors as anticancer agents.
Synthesis and antifungal activity of substituted salicylaldehyde hydrazones, hydrazides and sulfohydrazides
Backes, Gregory L.,Neumann, Donna M.,Jursic, Branko S.
, p. 4629 - 4636 (2014/11/08)
Efficient synthetic procedures for the preparation of acid hydrazines and hydrazides were developed by converting the corresponding carboxylic acid into the methyl ester catalyzed by Amberlyst-15, followed by a reaction with hydrazine monohydrate. Sulfohydrazides were prepared from the corresponding sulfonyl chlorides and hydrazine monohydrate. Both of these group of compounds were condensed with substituted salicylaldehydes using gradient concentration methods that generated a large library of hydrazone, hydrazide and sulfohydrazide analogs. Antifungal activity of the prepared analogs showed that salicylaldehyde hydrazones and hydrazides are potent inhibitors of fungal growth with little to no mammalian cell toxicity, making these analogs promising new targets for future therapeutic development.
Enhancers of protein degradation
-
Page/Page column 14, (2011/04/14)
The present invention relates to compounds suitable for modulating huntingtin protein processing and useful for treating or preventing huntingtin-related disorders. The invention provides pharmaceutical compositions comprising said compounds and methods of syntheses thereof.
ENHANCERS OF PROTEIN DEGRADATION
-
Page/Page column 25-26; 36, (2011/04/13)
The present invention relates to compounds suitable for modulating huntingtin protein processing and useful for treating or preventing huntingtin-related disorders. The invention provides pharmaceutical compositions comprising said compounds and methods of syntheses thereof.
