Based on a model of docked CAPE in AKR1B10, its derivatives were designed, synthesized and evaluated for inhibitory potency.
A series of N- 4-alkoxy-3-cyanophenyl)isoN- 4-alkoxy-3-cyanophenyl derivatives was desigN- 4-alkoxy-3-cyanophenyluated for iN- 4-alkoxy-3-cyanophenylo agaiN- 4-alkoxy-3-cyanophenyl
A small library of dihydropyrimidin-2-ones (DHPMs) was synthesized and evaluated for their potency to block iodide entrapment in rat thyroid cells.
New series of thiophene-containing phenoxypropanolamines were synthesized and evaluated for their potency to inhibit the three proteolytic activities of the mammalian 20S proteasome.
In the present work, thirty-one N2,N4-disubstituted quinazoline-2,4-diamines that had not previously been examined for their antileishmanial activity were evaluated for their potency and selectivity against Leishmania donovani, the causative parasite of visceral leishmaniasis.
Based on the pharmacological importance of dihydropyrimidine (DHPM) scaffold, substituted DHPMs linked with acetamide linker to substituted aromatic anilines were synthesized and evaluated for their potency as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors.
N- 5- 5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene 4-oxo-2-thioxo-1,3-thiazolidin-3-yl)N- 5- 5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene 4-oxo-2-thioxo-1,3-thiazolidin-3-yluated for iN- 5- 5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene 4-oxo-2-thioxo-1,3-thiazolidin-3-yl-state kiN- 5- 5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene 4-oxo-2-thioxo-1,3-thiazolidin-3-yl
A series of new taxoids modified at the C-3′, C-3′N, C-10, C-2 and C-7 positions has been designed, synthesized and evaluated for their potency to induce NO and TNF production by peritoneal murine macrophages (Mφ) from LPS-responsive C3H/HeN and LPS-hyporesponsive C3H/HeJ strains and human blood cells, and for their ability to inhibit the growth of Mφ-like cell lines J774.1 and J7.DEF3.
A few of the NPAHs and OPAHs have also been evaluated for mutagenic potency, and many of these exhibit genotoxicity with or without enzymatic activation (Durant et al. 1996).
Eleven selected compounds were evaluated for their inhibitory potency against p38α MAPK kinase.
