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New Quinoxaline Derivatives as Dual Pim-1/2 Kinase Inhibitors: Design, Synthesis and Biological Evaluation
| Content Provider | MDPI |
|---|---|
| Author | Logé, Cédric Oyallon, Bruno Brachet-Botineau, Marie Robert, Thomas Bach, Stéphane Ibrahim, Sajida Raoul, William Croix, Cécile Berthelot, Pascal Guillon, Jean Pinaud, Noël Gouilleux, Fabrice Viaud-Massuard, Marie-Claude Denevault-Sabourin, Caroline |
| Copyright Year | 2021 |
| Description | Proviral integration site for Moloney murine leukemia virus (Pim)-1/2 kinase overexpression has been identified in a variety of hematologic (e.g., multiple myeloma or acute myeloid leukemia (AML)) and solid (e.g., colorectal carcinoma) tumors, playing a key role in cancer progression, metastasis, and drug resistance, and is linked to poor prognosis. These kinases are thus considered interesting targets in oncology. We report herein the design, synthesis, structure–activity relationships (SAR) and in vitro evaluations of new quinoxaline derivatives, acting as dual Pim1/2 inhibitors. Two lead compounds (5c and 5e) were then identified, as potent submicromolar Pim-1 and Pim-2 inhibitors. These molecules were also able to inhibit the growth of the two human cell lines, MV4-11 (AML) and HCT-116 (colorectal carcinoma), expressing high endogenous levels of Pim-1/2 kinases. |
| Starting Page | 867 |
| e-ISSN | 14203049 |
| DOI | 10.3390/molecules26040867 |
| Journal | Molecules |
| Issue Number | 4 |
| Volume Number | 26 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2021-02-06 |
| Access Restriction | Open |
| Subject Keyword | Molecules Medicinal Chemistry Quinoxaline Pim Kinases Kinase Inhibitor Anticancer Targeted Therapy |
| Content Type | Text |
| Resource Type | Article |
