Conformationally constrained 6‑aryl‑1‑(3,4,5‑trimethoxyphenyl)-1H-pyrazolo[3,4‑b]pyrazines as novel microtubule destabilizers: design, synthesis, and antitumor evaluation

Novel 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine derivatives: design, synthesis, and biological evaluation as potent tubulin polymerisation inhibitors with anticancer activity

Mechanistic assays confirmed 9t serves as a promising dual-function tubulin inhibitor with both cytostatic and cytotoxic anticancer effects, meriting further preclinical investigation.

Design, synthesis, molecular docking and anticancer activity of novel N-(4-(chlorodifluoromethoxy)phenyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives

Results suggest that the N-(4-(chlorodifluoromethoxy)phenyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold is a useful template for designing selective BCR-ABL1-directed anticancer agents, with compound 9c as an encouraging lead for further optimisation and mechanistic studies.

Enhancement of antitumor activity through structural optimization of 2-(Benzylamino)-thieno[2,3-d]pyrimidin-4(3H)-ones

Discovery, Synthesis, and Biological Evaluation of 1,3,4,5-Tetrahydro-6H-pyrano[4,3-c]isoquinolin-6-one Derivatives as Novel and Highly Selective PARP1 Inhibitors.

(R)-A17, a novel, highly selective PARP1 inhibitor featuring a unique tricyclic scaffold, is developed and established as a promising candidate and the design strategy for the next-generation PARP1-targeted therapy is validated.

Novel [1,2,4]triazolo[1,5-a]pyrimidine derivatives as promising antioxidant and antimicrobial agents: Synthesis, antibiofilm, DFT calculations, molecular docking, ADMET analysis, and MD simulations.

The escalating threat of antimicrobial resistance necessitates the discovery of novel therapeutic scaffolds with distinct mechanisms of action. A novel series of [1,2,4]triazolo[1,5-a]pyrimidine derivatives (FNT01-12) featuring various aromatic substitutions at positions 5 and 7 was designed, synthesized, and evaluated...

Design, synthesis, and in vitro/in vivo evaluation of novel diphenyl-1,2,4-triazine-3-yl-thioacetamide-chalcone hybrids as potent α-glucosidase inhibitors targeting type 2 diabetes.

A novel series of 5,6-diphenyl-1,2,4-triazine-3-yl-thioacetamide-chalcone hybrids (9a-n) was designed, synthesized, and evaluated for their antidiabetic potential. All derivatives exhibited potent in vitro α-glucosidase inhibitory activity (IC50 = 0.2-112 μM) compared with acarbose (IC50 = 750.0 μM). The most potent co...