IM–chitosan complex encapsulated poly(ε-caprolactone) (PCL) nanoparticles are proposed for their potential in enabling more intelligent controlled release and enhancing chemotherapeutic efficiency of IM.
Isidro Cortés-Ciriano, Qurrat Ul Ain, Vigneshwari Subramanian, Eelke B. Lenselink, Oscar Méndez-Lucio, Adriaan P. IJzerman, Gerd Wohlfahrt, Peteris Prusis, Thérèse E. Malliavin, Gerard J. P. van Westen and Andreas Bender
A series of novel aryl triazoles was synthesized as firefly luciferase inhibitors in vitro and in vivo. More interestingly, these compounds are mixed noncompetitive for luciferin and noncompetitive for ATP.
A D-proline peptidomimetic targeting MMP-2 and MMP-9, being involved during tumor cell invasion and angiogenesis, was identified from a pool of compounds following enzyme inhibition kinetics and zymography, clearly highlighting...
Polymeric micelles for therapeutic delivery of hydrogen sulfide (H2S) were developed. The micelles released H2S in murine macrophages and enhanced proinflammatory responses induced by a Toll-like receptor 7 ligand, gardiquimod....
Hierarchical structure-based virtual screening against the sphingosine kinase 1(SphK1) binding pocket was performed. 25 compounds were selected for biological evaluation. Compound 25 exhibited comparable SphK1 and SphK2 inhibitory activities and anti-proliferative effects on U937 cells to the positive control N,N-dimethylsphingosine (DMS) 1. Further molecule dynamic (MD) simulations revealed the binding mode between SphK1 and 25.
Four novel series of 1-substituted-3-(2-methyl-4-oxo-4H-quinazolin-3-yl) urea and/or thiourea IIIa-c, 4-substituted-N-(2-methyl-4-oxo-4H-quinazolin-3-yl) benzene sulfonamide VIa-c and their NO-hybrid molecules as nitrate esters Va-c, VIIIa-c have been synthesized and evaluated for their anti-inflammatory...
To investigate the role of chirality in the ligand–σ1 receptor interaction, a series of enantiomeric arylalkylaminoalcohols and arylpyrrolidinols was evaluated by means of both in silico and in vitro studies.
Guilherme A. M. Jardim, Tiago T. Guimarães, Maria do Carmo F. R. Pinto, Bruno C. Cavalcanti, Kaio M. de Farias, Claudia Pessoa, Claudia C. Gatto, Divya K. Nair, Irishi N. N. Namboothiri and Eufrânio N. da Silva Júnior
Naphthoquinone-based chalcone hybrids were synthesized and evaluated for their cytotoxic activity against four cancer cell lines and PBMC. Some of the hybrids exhibited promising anticancer activity with IC50 values < 1 μM.