title: 7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.
abstract: A novel series of 7-[1H-indol-2-yl]-2,3-dihydro-isoindol-1-ones designed to be inhibitors of VEGF-R2 kinase was synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, and initial SAR of the series are discussed.
authors: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, PO Box 300, 1000 Route 202, Raritan, NJ 08869, USA. hughe007@hotmail.com
authors: Terry V
authors: TV
authors: Hughes
authors: Stuart L
authors: SL
authors: Emanuel
authors: Harold R
authors: HR
authors: O'Grady
authors: Peter J
authors: PJ
authors: Connolly
authors: Catherine
authors: C
authors: Rugg
authors: Angel R
authors: AR
authors: Fuentes-Pesquera
authors: Prabha
authors: P
authors: Karnachi
authors: Richard
authors: R
authors: Alexander
authors: Steven A
authors: SA
authors: Middleton
mesh_terms: D000818:Animals; D064096:Aurora Kinase A; D064127:Aurora Kinases; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D042442:Vascular Endothelial Growth Factors / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays
chemical_list: D007211:Indoles; D042442:Vascular Endothelial Growth Factors; D020794:Receptor Protein-Tyrosine Kinases; C576918:Aurka protein, mouse; D064096:Aurora Kinase A; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases