Design, synthesis and biological evaluation of type-II VEGFR-2 inhibitors based on quinoxaline scaffold
Shahin, Mai I; Abou El Ella, Dalal; Ismail, Nasser S M; Abouzid, Khaled;
Abstract
In an effort to develop ATP-competitive VEGFR-2 selective inhibitors, a series of new quinoxaline-based derivatives was designed and synthesized. The target compounds were biologically evaluated for their inhibitory activity against VEGFR-2. The design of the target compounds was accomplished after a profound study of the structure activity relationship (SAR) of type-II VEGFR-2 inhibitors. Among the synthesized compounds, 1-(2-((4-methoxyphenyl)amino)-3-oxo-3,4 dihydroquinoxalin-6-yl)-3-phenylurea (VIIa) displayed the highest inhibitory activity against VEGFR-2. Molecular modeling study involving molecular docking and field alignment was implemented to interpret the variable inhibitory activity of the newly synthesized compounds.
Other data
| Title | Design, synthesis and biological evaluation of type-II VEGFR-2 inhibitors based on quinoxaline scaffold | Authors | Shahin, Mai I; Abou El Ella, Dalal ; Ismail, Nasser S M; Abouzid, Khaled | Keywords | Docking study;Kinase;Quinoxaline;Type-II;VEGFR-2 | Issue Date | Oct-2014 | Publisher | ACADEMIC PRESS INC ELSEVIER SCIENCE | Journal | Bioorganic Chemistry | Volume | 56 | Start page | 16 | End page | 26 | ISSN | 0045-2068 | DOI | 10.1016/j.bioorg.2014.05.010 | PubMed ID | 24922538 | Scopus ID | 2-s2.0-84902130038 | Web of science ID | WOS:000341425600003 |
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