Bassem H. Naguib1,2 and Hala B. El-Nassan2
1Pharmaceutical Chemistry Department, Faculty of Pharmacy, The British University in Egypt BUE, Cairo 11837, Egypt; 2Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt
Pim Kinases have emerged as a novel therapeutic molecular target affiliated with different types of malignancy. Three series of 5-bromo-thieno[2, 3-b] pyridine analogs bearing amide or benzoyl groups at position – 2 were synthesized, followed by cytotoxicity screening against five cell lines [MCF7, HEPG2, HCT116, A549, and PC3], representing different types of cancer. The synthesized analogs were biologically evaluated for their pim-1 enzyme inhibitory activity, where two analogs (3c and 5b) showed potent pim-1 inhibitory activity with IC50 of 35.70 and 12.71 µM, respectively. Another three analogs (3d, 3g and 6d) showed moderate pim-1 inhibition. This would offer a viable route for further development novel analogs targeting pim-1 kinase.
Keywords: Thieno[2,3-b]pyridine; cytotoxic activity; pim-1.