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2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: a structure-activity relationship study |
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| Authors: | Chen Qianyi Bryant Vashti C Lopez Hernando Kelly David L Luo Xu Natarajan Amarnath |
| Affiliation: | a Eppley Institute for Cancer Research, University of Nebraska Medical Center, Omaha, NE 68198, United States b Department of Genetics, Cell Biology and Anatomy, University of Nebraska Medical Center, Omaha, NE 68198, United States c Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States |
| Abstract: | The quinoxaline core is considered a privileged scaffold as it is found in a variety of biologically relevant molecules. Here we report the synthesis of a quinoxalin-6-amine library, screening against a panel of cancer cell lines and a structure-activity relationship (SAR). This resulted in the identification of a bisfuranylquinoxalineurea analog (7c) that has low micromolar potency against the panel of cancer cell lines. We also show that cells treated with quinoxalineurea 7c results in caspase 3/7 activation, PARP cleavage and Mcl-1 dependent apoptosis. |
| Keywords: | Quinoxaline urea Antiproliferative Mcl-1 dependent apoptosis |
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