Journal of Medicinal Chemistry p. 1649 - 1667 (2008)
Update date:2022-08-30
Topics:
Harmange, Jean-Christophe
Weiss, Matthew M.
Germain, Julie
Polverino, Anthony J.
Borg, George
Bready, James
Chen, Danlin
Choquette, Deborah
Coxon, Angela
DeMelfi, Tom
DiPietro, Lucian
Doerr, Nicholas
Estrada, Juan
Flynn, Julie
Graceffa, Russell F.
Harriman, Shawn P.
Kaufman, Stephen
La, Daniel S.
Long, Alexander
Martin, Matthew W.
Neervannan, Sesha
Patel, Vinod F.
Potashman, Michele
Regal, Kelly
Roveto, Phillip M.
Schrag, Michael L.
Starnes, Charlie
Tasker, Andrew
Teffera, Yohannes
Wang, Ling
White, Ryan D.
Whittington, Douglas A.
Zanon, Roger
A series of naphthyl-based compounds were synthesized as potential inhibitors of vascular endothelial growth factor (VEGF) receptors. Investigations of structure-activity relationships led to the identification of a series of naphthamides that are potent inhibitors of the VEGF receptor tyrosine kinase family. Numerous analogues demonstrated low nanomolar inhibition of VEGF-dependent human umbilical vein endothelial cell (HUVEC) proliferation, and of these several compounds possessed favorable pharmacokinetic (PK) profiles. In particular, compound 48 demonstrated significant antitumor efficacy against established HT29 human colon adenocarcinoma xenografts implanted in athymic mice. A full account of the preparation, structure-activity relationships, pharmacokinetic properties, and pharmacology of analogues within this series is presented.
View MoreContact:18669908765
Address:Zibo City, Shandong Province, P.R.China
Zhejiang Chemline International Co., Ltd.
Contact:+86-571-88062298
Address:Hengdian Industry Area, Dongyang, Zhejiang, China
Wuxi Innopal International Trade CO.,LTD
Contact:+86-510-80711901-8003
Address:Room 402,Building 5,Longze Garden,No.17,South huanjiu Road,Yixing City, Jiangsu,China
Contact:+86-0512-69209969
Address:Room 317,Lushan Road,Suzhou New District,Jiangsu Province,China.
Chengdu Boon Stream Chemical Industry Co.,Ltd.
Contact:+86-28-83156758
Address:No.859,Dongzikou Road,Jinniu District,Chengdu,Sichuan,P.R.China
Doi:10.1080/00397911.2013.839795
(2014)Doi:10.1021/jacs.6b04425
(2016)Doi:10.1055/s-2006-951520
(2006)Doi:10.1021/jacs.7b05448
(2017)Doi:10.1007/s10600-009-9246-9
(2009)Doi:10.1016/S0040-4039(01)02148-7
(2002)