10.1016/j.bioorg.2019.102988
The study focuses on the design, synthesis, and biological evaluation of a novel chemical scaffold, 6,7-dihydro-5H-cyclopenta[d]pyrimidine derivatives, as inhibitors of vascular endothelial growth factor receptor 2 (VEGFR 2). The research involved molecular modeling protocols, including 3D-QSAR pharmacophore modeling, virtual screening, and docking studies, to identify and design potential VEGFR 2 inhibitors. The chemicals used in the study include a series of synthesized 6,7-dihydro-5H-cyclopenta[d]pyrimidine derivatives, with compounds 6c and 6b showing significant enzyme inhibition of 97% and 87% at 10 μM, respectively. These compounds were designed to target the VEGFR 2 receptor, which plays a crucial role in angiogenesis and is a key therapeutic target for inhibiting tumor growth and metastasis. The purpose of these chemicals was to serve as potential anti-cancer agents by inhibiting the VEGFR 2 signaling pathway, thereby affecting the blood supply to tumor cells and inhibiting their growth and spread.
10.1021/ol050975u
The research aims to synthesize the branched C-glycoside substructure of altromycin B, an antibiotic and anticancer compound, using non-carbohydrate precursors. The study employs a tungsten-catalyzed cycloisomerization of alkynyl alcohols to produce key intermediates, followed by a sequence of Stille cross-coupling reactions and selective functional group transformations. Key chemicals used include alkynyl alcohols such as 8, tungsten hexacarbonyl (W(CO)?), and various reagents for functional group transformations like DIBAL (diisobutylaluminum hydride), TBSCl (tert-butyldimethylsilyl chloride), and AD-mix (Sharpless asymmetric dihydroxylation reagent). The research concludes with the successful synthesis of the C13-diastereomers of the branched C-arylglycoside (2a and 2b), which were confirmed by X-ray crystallography and NMR spectroscopy. The findings support ongoing efforts towards the total synthesis of altromycin natural products and provide a robust synthetic route for this complex substructure.
