Structure Activity Relationship Studies around <i><named-content content-type="color:blue">DB18</named-content></i>, a Potent and Selective Inhibitor of CLK Kinases

Structure Activity Relationship Studies around <i><named-content content-type="color:blue">DB18</named-content></i>, a Potent and Selective Inhibitor of CLK Kinases

Three series of our lead CLK1 inhibitor <b><i>DB18</i></b> have been designed, synthetized and tested against CLKs and DYRK1A kinases. Their cytotoxicity was subsequently measured on seven representative cancer cell lines. Guided by docking experiments, we focused on the less...

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Bibliographic Details
Main Authors: Dabbugoddu Brahmaiah, Anagani Kanaka Durga Bhavani, Pasula Aparna, Nangunoori Sampath Kumar, Hélène Solhi, Rémy Le Guevel, Blandine Baratte, Thomas Robert, Sandrine Ruchaud, Stéphane Bach, Surender Singh Jadav, Chada Raji Reddy, Paul Mosset, Nicolas Gouault, Nicolas Levoin, René Grée
Format: Article
Language:English
Published: MDPI AG 2022-09-01
Series:Molecules
Subjects:
kinases
CLK-kinases
DYRK1A kinase
quinazoline
cytotoxicity
molecular modelling
Online Access:https://www.mdpi.com/1420-3049/27/19/6149

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https://www.mdpi.com/1420-3049/27/19/6149

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