title: Solution phase parallel synthesis and evaluation of MAPK inhibitory activities of close structural analogues of a Ras pathway modulator.
abstract: A solution phase parallel synthesis approach was undertaken to rapidly explore the structure-activity relationship of an inhibitor of the Ras/Raf protein interaction identified from a small molecule compound library. Evaluation of the MAPK pathway signaling inhibitory activity of the synthesized analogues as well as their antiproliferative activity and ability to inhibit soft agar growth were performed.
authors.affiliation: Morphochem Inc., 11 Deer Park Drive, Suite 116, Monmouth Junction, NJ 08852, USA.
authors.forename: Yingchun
authors.initials: Y
authors.lastname: Lu
authors.forename: Sukumar
authors.initials: S
authors.lastname: Sakamuri
authors.forename: Quin-Zene
authors.initials: QZ
authors.lastname: Chen
authors.forename: Yen-Fang
authors.initials: YF
authors.lastname: Keng
authors.forename: Vladimir
authors.initials: V
authors.lastname: Khazak
authors.forename: Katrin
authors.initials: K
authors.lastname: Illgen
authors.forename: Silke
authors.initials: S
authors.lastname: Schabbert
authors.forename: Lutz
authors.initials: L
authors.lastname: Weber
authors.forename: Sanjay R
authors.initials: SR
authors.lastname: Menon
mesh_terms: D000818:Animals; D016466:CHO Cells; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D006224:Cricetinae; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D020928:Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship; D018631:ras Proteins / Q000037:antagonists & inhibitors*; D003986:Dibenzocycloheptenes
chemical_list: D004791:Enzyme Inhibitors; D020928:Mitogen-Activated Protein Kinases; D010880:Piperidines; D011725:Pyridines; D011994:Recombinant Proteins; D018631:ras Proteins; C115354:lonafarnib; D003986:Dibenzocycloheptenes