title: Synthesis and in vivo evaluation of N-ethylamino-2-oxo-1,2-dihydro-quinoline-3-carboxamide for inhibition of intestinal tumorigenesis in APC(Min/+) mice.
abstract: A selective KGFR tyrosine kinase inhibitor, N-ethylamino-2-oxo-1,2-dihydro-quinoline-3-carboxamide, was synthesized and its possible inhibitory effects on the development of colon polyps and colorectal tumors was examined in APC(Min/+) mice, a mouse model of human intestinal familial adenomatous polyposis. The present study shows for the first time that a dietary administration of a selective KGFR tyrosine kinase inhibitor lacks the overt-toxicities and significantly reduced the growth of small intestinal polyps in both male and female APC(Min/+) mice. This inhibition of polyp growth appears to occur at a greater extent in female mice.
authors: Department of Pharmaceutical Sciences, College of Pharmacy, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA; Hematology/Oncology Section, Department of Internal Medicine, College of Medicine, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA.
authors: Gopal
authors: G
authors: Pathuri
authors: Hematology/Oncology Section, Department of Internal Medicine, College of Medicine, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA; Center for Cancer Prevention and Drug Development, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA.
authors: Qian
authors: Q
authors: Li
authors: Hematology/Oncology Section, Department of Internal Medicine, College of Medicine, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA; Center for Cancer Prevention and Drug Development, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA.
authors: Altaf
authors: A
authors: Mohammed
authors: Department of Pharmaceutical Sciences, College of Pharmacy, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA; Experimental Therapeutics Program, Peggy and Charles Stephenson Oklahoma Cancer Center, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA.
authors: Hariprasad
authors: H
authors: Gali
authors: Department of Pharmaceutical Sciences, College of Pharmacy, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA; Experimental Therapeutics Program, Peggy and Charles Stephenson Oklahoma Cancer Center, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA. Electronic address: tom-pento@ouhsc.edu.
authors: J Thomas
authors: JT
authors: Pento
authors: Hematology/Oncology Section, Department of Internal Medicine, College of Medicine, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA; Center for Cancer Prevention and Drug Development, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, USA.
authors: Chinthalapally V
authors: CV
authors: Rao
mesh_terms: D011125:Adenomatous Polyposis Coli / Q000188:drug therapy; D000577:Amides / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D063646:Carcinogenesis / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy; D004195:Disease Models, Animal; D005260:Female; D006801:Humans; D008297:Male; D051379:Mice; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D011804:Quinolines / Q000737:chemistry*; D051497:Receptor, Fibroblast Growth Factor, Type 2 / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011804:Quinolines; C037219:quinoline; D051497:Receptor, Fibroblast Growth Factor, Type 2; C065104:keratinocyte growth factor receptor
keywords: Chemoprevention; Colon cancer; KFGR; Polyps; Tyrosine kinase inhibitor