A tenascin-C derived peptide (TNIIIA2 peptide, 1) stimulated beta 1 integrin-mediated cell adhesion via binding to syndecan-4. Ala-substituted peptides were synthesized to understand the structure-activity relationship. ...
A series of hydroxyalkyl and acyloxyalkyl derivatives of 2- and 3-hydroxypyridine was synthesized and their biological activity was evaluated as growth inhibitors of protozoan Leishmania mexicana. Thirty novel compounds ...
Accumulation of misfolded alpha-synuclein in Lewy bodies and Lewy neurites is the pathological hallmark of Parkinson's disease (PD). To identify ligands having high binding potency toward aggregated alpha-synuclein, we s...
PARP-1, the most abundant member of the PARP superfamily of nuclear enzymes, has emerged as a promising molecular target in the past decade particularly for the treatment of cancer. A number of PARP-1 inhibitors, includi...
A high throughput in vitro screen has been developed to identify substances that induce expression of C/EBP alpha in tumor cells. An extract of the fruit of Gyrocarpus jacquinii showed induction of C/EBP alpha activity t...
Methicillin-resistant Staphylococcus aureus (MRSA) poses a serious threat to public health because of its resistance to multiple antibiotics most commonly used to treat infection. In this study, we report the unique abil...
A series of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives (Ia-Il) were synthesized and biologically evaluated. It was found that Ig, the most active compound, antagonized both Ang II AT(1) and endothe...
The F-19 NMR probes for the HNO detection are reported. We synthesized the probe molecules with the paramagnetic Cu(II) complex and fluorine atoms using a cubic silsesquioxane. By using the magnetism changes of the Cu(II...
We report the tumor cell-selective prodrugs based on the arsonic acid-presenting iron oxide nanoparticles. We synthesized the well-dispersed nanoparticles having arsonoacetic acid which is composed of the low toxic As(V)...
As an alternative to the previously reported solid dispersion formulation for enhancing the oral absorption of thiazolo[5,4-b]pyridine 1, we investigated novel N-acyl imide prodrugs of 1 as RAF/vascular endothelial growt...
Two half-sandwich cobalt and rhodium complexes 2a and 2b with combination of carborane and N-Sulfonamide were synthesized and fully characterized by NMR spectroscopy, mass spectrometry, elemental analysis as well as X-ra...
In this study, a series of 11 10-aminoethylether derivatives of artemisinin were synthesised and their antimalarial activity against both the chloroquine sensitive (D10) and resistant (Dd2) strains of Plasmodium falcipar...
Methylated analogues of imidazoline related compounds (IRC) were prepared; their abilities to bind I-1 imidazoline receptors (I(1)Rs), I-2 imidazoline binding sites (I2BS) and alpha(2)-adrenoceptor subtypes (alpha(2)ARs)...
Herein we describe the diastereoselective synthesis of glutamic acid analogs and the evaluation of their agonist activity towards metabotropic glutamate receptor subtype 4 (mGluR4). These analogs are based on a monofluor...
New analogues of N-acyl-homoserine-lactone (AHL), in which the amide was replaced by a triazole or tetrazole ring, were prepared and tested for their activity as LuxR-dependent QS modulators. Several compounds showed a l...
Acylhomoserine lactone (AHL) analogues in which the amide function is replaced by a triazole group were synthesized and evaluated for their effect on quorum sensing (QS) and biofilm formation in Burkholderia cenocepacia ...