Antiangiogenic Effects of VH02, a Novel Urea Derivative: In Vitro and in Vivo Studies.

Vascular endothelial growth factor receptor 2 (VEGFR2) is a vital target for therapeutic intervention in cancer. We have recently described a computer-based drug design for a small molecule VEGFR2 inhibitor named VH02 (1-((1-(1-indazol-6-yl)-1-1,2,3-triazol-4-yl)methyl)-3-(3-chloromethylphenyl)urea). This study aimed to further explore the anti-angiogenic activity of VH02 both in vitro and in vivo.

Novel VEGFR-2 kinase inhibitors identified by the back-to-front approach.

We report a novel VEGFR-2 inhibitor, developed by the back-to-front approach. Docking experiments indicated that the 3-chloromethylphenylurea motif of the lead compound occupied the back pocket of VEGFR-2 kinase. An attempt was made to enhance the binding affinity of 1 by expanding the structure to access the front pocket using a triazole linker.

Insecticidal activity of Jatropha gossypifolia L. (Euphorbiaceae) and Cleome viscosa L. (Capparidacae) on Spodoptera litura (Lepidoptera: Noctuidae). Toxicity and carboxylesterase and glutathione-S-transferase activities studies.

The naturally occurring phytocidal chemical components of some Thai plant-species are responsible for controlling and repelling insects from the host plants. The aim of this study was to evaluate the insecticidal activity of Jatropha gossypifolia L. Leaf extracts and the senescent leaf Cleome viscosa L.