dc.contributor.author |
Szabadkai, I |
|
dc.contributor.author |
Torka, R |
|
dc.contributor.author |
Garamvölgyi, Rita |
|
dc.contributor.author |
Baska, Ferenc |
|
dc.contributor.author |
Gyulavári, Pál |
|
dc.contributor.author |
Boros, Sándor |
|
dc.contributor.author |
Illyes, E |
|
dc.contributor.author |
Choidas, A |
|
dc.contributor.author |
Ullrich, A |
|
dc.contributor.author |
Őrfi, László |
|
dc.date.accessioned |
2020-04-09T08:09:40Z |
|
dc.date.available |
2020-04-09T08:09:40Z |
|
dc.date.issued |
2018 |
|
dc.identifier.citation |
journalVolume=61;journalIssueNumber=14;journalTitle=JOURNAL OF MEDICINAL CHEMISTRY;pagerange=6277-6292;journalAbbreviatedTitle=J MED CHEM; |
|
dc.identifier.uri |
http://repo.lib.semmelweis.hu//handle/123456789/7583 |
|
dc.identifier.uri |
doi:10.1021/acs.jmedchem.8b00672 |
|
dc.description.abstract |
The overexpression of AXL kinase has been described in many types of cancer. Due to its role in proliferation, survival, migration, and resistance, AXL represents a promising target in the treatment of the disease. In this study we present a novel compound family that successfully targets the AXL kinase. Through optimization and detailed SAR studies we developed low nanomolar inhibitors, and after further biological characterization we identified a potent AXL kinase inhibitor with favorable pharmacokinetic profile. The antitumor activity was determined in xenograft models, and the lead compounds reduced the tumor size by 40% with no observed toxicity as well as lung metastasis formation by 66% when compared to vehicle control. |
|
dc.format.extent |
6277-6292 |
|
dc.relation.ispartof |
urn:issn:0022-2623 |
|
dc.title |
Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors |
|
dc.type |
Journal Article |
|
dc.date.updated |
2019-09-03T14:25:46Z |
|
dc.language.rfc3066 |
en |
|
dc.rights.holder |
NULL |
|
dc.identifier.mtmt |
3408491 |
|
dc.identifier.wos |
000440521300031 |
|
dc.identifier.pubmed |
29928803 |
|
dc.contributor.department |
SE/AOK/I/Orvosi Vegytani, Molekuláris Biológiai és Patobiokémiai Intézet |
|
dc.contributor.department |
SE/GYTK/Gyógyszerészi Kémiai Intézet |
|
dc.contributor.institution |
Semmelweis Egyetem |
|