In an attempt to develop potent and selective anticancer agents, some 5‐ or 6‐ and N‐substituted benzoxazol‐2‐carboxamide derivatives were designed, synthesized, and evaluated for their cyclooxygenase inhibitory, antioxidant, and anti‐proliferative activity against MCF‐7 and MDA‐MB‐231 cell lines. Among them 5‐OMe, N‐piperidine substituted (compound 30 ), 5‐OMe, N‐4‐methylpiperidine substituted (compound 31 ) and 5‐Cl, N‐piperidine substituted (compound 34 ) benzoxazole 2‐carboxamide compounds have a moderate inhibitory effect in COX‐1 and COX‐2 enzymes. Anti‐proliferative studies show that compound 30 (IC ₅₀ =5.35 μM) and compound 31 (IC ₅₀ =5.82 μM) have similar activity to reference drug 5‐FU (IC ₅₀ =3.95 μM) on MCF‐7 cell but they have lower toxic effect for healthy WI‐38 cell line. For the MCF‐7 cell line, compounds 30 and 31 show approximately 1.5 times higher selectivity compared to the 5‐FU control. Among the synthesized compounds 30 , 31 , and 34 had the best anti‐proliferative effect and were used to perform flow cytometry and cell cycle analysis on MCF‐7 cell line. To predict the binding modes and pharmacokinetic parameters of all compounds, in silico studies were carried out. These compounds may shed light on cancer treatment and cancer research.

Background: Phortress produces reactive electrophilic metabolites that form DNA adducts only in sensitive tumor cells. The authors converted the 2-phenylbenzothiazole nucleus in phortress to 2-aryl... Plain language summary There is an urgent need to develop potent and selective anticancer agents. In this study, the design and applications of compounds sensitive to specific cancer cells and targ...

In this study, a series of imidazo[1,2-a]pyridine-mannich bases were designed and synthesized for the inhibition of cholinesterases, one of the important pathways in the treatment of Alzheimer's dementia. The imidazopyridine scaffold, which is found in the structure of many active compounds in pharmaceutical use, is derived from Mannich-bases containing morpholine and various aromatic groups. In vitro AChE and BChE enzyme activities and enzyme kinetics studies of new potential drug candidates (9a-j) that can target the critical binding regions of cholinesterases were conducted. In vitro evaluation with donepezil, tacrine (control compounds), and 9a-j, it was found that naphthalene-substituted compound 9j exhibited the most potential anti-cholinesterase activity (IC₅₀s: 57.75 nM for AChE; 99.0 nM for BChE). Molecular docking studies performed with hAChE and hBChE enzyme crystal structures revealed that compound 9j has a higher binding affinity by targeting the CAS and PAS binding sites. Additionally, drug-likeness and pre-ADMET evaluation of the compounds showed that compound 9j had the most favorable drug properties. These results might be a new milestone in terms of the promising importance of the imidazopyridine scaffold in future drug design for the treatment of AD. Graphical abstract