Synthesis of novel 1-aryl-3-[2,3- or 4-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas and evaluation as VEGFR2 tyrosine kinase inhibitors

Peixoto, Daniela; Queiroz, Maria João R.P.; Abreu, Rui M.V.; Froufe, Hugo J.C.; Calhelha, Ricardo C.; Ferreira, Isabel C.F.R.

http://hdl.handle.net/10198/7835

Use this identifier to reference this record.

Name:	Description:	Size:	Format:
Poster Int. 74-cópia 2.pdf		749.74 KB	Adobe PDF	Download

Send Feedback

Authors

Peixoto, Daniela

Queiroz, Maria João R.P.

Abreu, Rui M.V.

Froufe, Hugo J.C.

Calhelha, Ricardo C.

Ferreira, Isabel C.F.R.

Abstract(s)

Vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase is involved in cancer and in angiogenesis. Herein, we report the synthesis of novel1-aryl-3-[2-, 3- or 4-{thieno[3,2-b ]pyridin-7-ylthio) phenyl]ureas as VEGFR2 inhibitors by promoting the regioselective attack of the thiol group of the 4-aminothiophenol in the chlorine nucleophilic displacement on 7-chlorothieno[3,2-b]pyridine 1, obtaining the aminated compounds Za- c. These were reacted with arylisocyanates to give the corresponding 1,3-diarylureas 3a-c, 4a-c and Sa-c (see scheme).

URI

http://hdl.handle.net/10198/7835

Citation

Peixoto, Daniela; Queiroz, Maria João; Abreu, Rui M.V.; Froufe, Hugo; Calhelha, Ricardo C.; Ferreira, Isabel C.F.R. (2012). Synthesis of novel 1-aryl-3-[2,3- or 4-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas and evaluation as VEGFR2 tyrosine kinase inhibitors. In XXIInd International Symposium on Medicinal Chemistry. Berlin