Synthesis of Styryl-phenyl-ureas as Dual-targeted Inhibitors of PD-L1 and VEGFR-2
     
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Synthesis of Styryl-phenyl-ureas as Dual-targeted Inhibitors of PD-L1 and VEGFR-2

Styryl-phenyl-ureas as Perspective Inhibitors of PD-L1 and VEGFR-2Programmed death-ligand 1 (PD-L1, cluster of differentiation 274, CD274, B7 homolog 1 or B7-H1) is a transmembrane protein that plays a major role in suppressing the adaptive arm of immune system during particular events such as tissue allografts, pregnancy, autoimmune disease and some other pathological disease states. Upregulation of PD-L1 may allow cancers to evade the host immune system.

Vascular endothelial growth factor receptor 2 (VEGFR-2, Kinase insert domain receptor, KDR, CD309, FLK1) is a VEGF receptor that plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Abnormal functioning of VEGFR-2 is associated with cancer.

We offer the chemical optimization service - synthesis of targets-specific set of styryl-phenyl-urea derivatives as dual-targeted inhibitors of PD-L1 and VEGFR-2. These novel compounds will be selected from a set of 3,000+ virtual styryl-phenyl-ureas using our company’s proprietary molecular modeling platform, synthesized and provided for your biological projects.

This set of novel analogs will be synthesized exclusively upon your request.

This is referred to a paper from European Journal of Medicinal Chemistry* which showed that authors designed and evaluated styryl-phenyl-ureas as dual-targeted inhibitors of PD-L1 and VEGFR-2 in order to overcome resistance phenomena offered by cancer. Compound T.14 ((E)-1-(4-chlorophenyl)-3-(3-(4-methoxystyryl)phenyl)urea) shows the best antiangiogenic and immunomodulator properties:

Styryl-phenyl-ureas as Perspective Inhibitors of PD-L1 and VEGFR-2

Compound T.14
 
Design and synthesis of compounds with both anti-PD-L1 and anti-angiogenic effect is a promising direction in cancer treatment.
 

* Laura Conesa-Milián, Eva Falomir, Juan Murga, Miguel Carda, J. Alberto Marco. Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. Eur. J. Med. Chem. 2019, Vol. 170, pp. 87−98, DOI: 10.1016/j.ejmech.2019.03.012.

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