Synthesis and Biological Evaluation of Aziridin-1-Yl Oxime-Based Vorinostat Analogs as Anticancer Agents

The suberoyl anilide hydroxamic acid (vorinostat) analogs with the aziridin-1-yl oxime moiety as a possible metal chelating functionality have been synthesized. Their biological activity and stability under physiological conditions have been evaluated. Although some of the synthesized compounds demonstrated high antiproliferative activity against human HT1080 fibrosarcoma (HT1080, IC<inf>50</inf> 0.3–7.7 μM) comparable to vorinostat (HT1080, IC<inf>50</inf> 2.4 μM), they showed only weak histone deacetylase inhibition activity in HeLa cell line extracts

CCDC 827537: Experimental Crystal Structure Determination

An entry from the Cambridge Structural Database, the worlds repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures

Synthesis and MMP-2 Inhibition Studies of Novel Aziridine and Azetidine Derivatives

Matrix metalloproteinases (MMPs) are zinc-dependent endopeptidases that are responsible for cleavage of extracellular matrix proteins. Because of their effect on both physiological and pathological processes, MMPs have become interesting targets for treatment of cancer. In addition, it is known that MMP-2 has the most important impact to tumor growth. Based on previous research, new series of aziridine and azetidine derivatives containing 1,4-disubstituted 1,2,3-triazole in the side chain as well as aziridine derivatives containing 1,5-disubstituted 1,2,3-triazole in the side chain were synthesized using transition metals catalyzed Huisgen 1,3-dipolar cycloaddition. MMP-2 inhibition studies of target compounds revealed some promising results among aziridine derivatives containing 1,4-disubstituted 1,2,3-triazole, while for other two series inhibition potency was not detected

Synthesis and Evaluation of Reducing Capacity and Calcium Channel Blocking Activity of Novel 3,5-Dipropargylcarbonyl-Substituted 1,4-Dihydropyridines

Novel pyridinium salts on the basis of 4-(3-pyridyl)-3,5-dipropargylcarbonyl-1,4-dihydropyridine were obtained by quaternisation of pyridine moiety with different alkyl halides. The reducing capacity of the synthesized compounds was evaluated using phosphomolybdenum complex method. The obtained results confirmed that all tested compounds possessed reducing capacity. Callcium channel antagonist and agonist activities of the compounds were additionaly assayed by changes in intracellular calcium ion concentration in H9C2 and A7R5 cell lines. The obtained data confirmed that all synthesized 1,4-dihydropyridine derivatives have smouth muscle selective antagonist activities, and in the case of 4-phenyl derivative the activity was 4.7 times higher than that of amlodipine