Structural-based design, synthesis, and antitumor activity of novel alloxazine analogues with potential selective kinase inhibition

• Published in: European journal of medicinal chemistry Vol. 152; pp. 31 - 52
• Main Authors: Malki, Waleed H., Gouda, Ahmed M., Ali, Hamdy E.A., Al-Rousan, Rabaa, Samaha, Doaa, Abdalla, Ashraf N., Bustamante, Juan, Abd Elmageed, Zakaria Y., Ali, Hamed I.
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 25.05.2018; Elsevier
• Subjects: Alloxazine; Antitumor; Apoptosis; Chemistry, Medicinal; Docking; Kinase inhibitor; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Science & Technology; Alloxazine; Docking; Kinase inhibitor; Antitumor; Apoptosis; SRC FAMILY KINASE; ASSAY; 5-DEAZAFLAVIN DERIVATIVES; MOLECULAR DOCKING; BREAST-CANCER; APOPTOTIC CELLS; IMATINIB; LEUKEMIA-CELLS; RESISTANCE; EXPRESSION

Protein kinases are promising therapeutic targets for cancer therapy. Here, we applied multiple approaches to optimize the potency and selectivity of our reported alloxazine scaffold. Flexible moieties at position 2 of the hetero-tricyclic system were incorporated to fit into the ATP binding site an...