Join date: May 18, 2022


Uniop Designer 6: Software --> DOWNLOAD

Uniop Designer 6: Software --> DOWNLOAD

A: You may not be the only person to have this issue. The oldest version of the designer that I could find was version 5. If you don't already have a version 6 designer, then you can download it from the Exor site for free. To download, open the file by clicking on it and select Save as. If you want to install the designer on a different drive, then select the drive as the destination. Synthesis and potent anti-angiogenic activity of novel 3-alkyl-5-acyl-2-aryl-1,3,4-oxadiazoles as potent anti-angiogenic agent. Oxadiazole and triazole compounds are known to have potent anti-angiogenic activity. Here, we describe the synthesis and biological activity of a new series of 3-alkyl-5-acyl-2-aryl-1,3,4-oxadiazoles as potent anti-angiogenic agents. We synthesized 15 target compounds, out of which 10 compounds showed moderate to good anti-angiogenic activity. Furthermore, anti-angiogenic assay using human umbilical vein endothelial cells (HUVEC) showed that all the compounds except 3-alkyl-5-cyanopentyl-2-aryl-1,3,4-oxadiazoles had excellent inhibitory activity. The most potent compound, 4-{4-[(5-bromo-2-methoxyphenyl)-(5-ethyl-2-phenyl-1,3,4-oxadiazol-4-yl)methoxy]benzoyl}-2-methylbenzoic acid (IC50: 0.95 ± 0.09 μM) showed a comparable potency to the lead compound EG4063. Structure-activity relationship (SAR) analyses indicated that the 4-hydroxyl group at R1 and the 3-alkyl group at R2 position were essential for anti-angiogenic activity. Moreover, hydrophobic substituents in R2 position, such as fluoro, chloro and bromo, enhanced the anti-angiogenic activity. The potential anti-angiogenic activity of the most potent compound could be further improved by replacing the aromatic group at R3 position with alkyl and/or phenyl groups. The most potent compound also inhibited the growth of human tumor cell


Uniop Designer 6: Software ~UPD~

More actions