861877-51-2Relevant academic research and scientific papers
Small molecules with potent osteogenic-inducing activity in osteoblast cells
Han, Chun-Ya E.,Wang, Youping,Yu, Longchuan,Powers, David,Xiong, Xiaoling,Yu, Violeta,Nguyen, Yen,Jean Jr., David J. St.,Babij, Philip
, p. 1442 - 1445 (2009)
A chemical screen of 45,000 compounds from a diverse collection led to the identification of two series of small molecules with potent osteogenic activity in mouse MC3T3-E1 osteoblast cells. The first chemical group was characterized by an amino benzothia
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: Design, synthesis, and evaluation
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
, p. 1649 - 1667 (2008/09/20)
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.
