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

• Main Authors: Kingkan Sanphanya, Suvara K. Wattanapitayakul, Suwadee Phowichit, Valery V. Fokin, Opa Vajragupta
• Other Authors: Mahidol University
• Format: Article
• Published: 2018
• Subjects: Biochemistry, Genetics and Molecular Biology; Chemistry; Pharmacology, Toxicology and Pharmaceutics
• Online Access: https://repository.li.mahidol.ac.th/handle/123456789/31310

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...