- Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors
-
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.
- Szabadkai, István,Torka, Robert,Garamv?lgyi, Rita,Baska, Ferenc,Gyulavári, Pál,Boros, Sándor,Illyés, Eszter,Choidas, Axel,Ullrich, Axel,órfi, László
-
p. 6277 - 6292
(2018/07/05)
-
- Quinolinyloxyphenylsulfonamides
-
The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions conta
- -
-
Page/Page column 38-39
(2011/05/04)
-
- QUINOLINYLOXYPHENYLSULFONAMIDES
-
The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.
- -
-
Page/Page column 66; 67
(2011/05/05)
-