Novel Dorsomorphin Derivatives: Molecular Modeling, Synthesis, and Bioactivity Evaluation.

ABSTRACT: Dorsomorphin, a pyrazolo[1,5-a]pyrimidine derivative, inhibits the bone morphogenetic protein (BMP) pathway by targeting the type I BMP receptors active in receptor-like kinases. However, the investigation of its-and its derivatives'-antiproliferative activity towards endothelial and cancer cell lines still requires reinforcement with additional studies. In the presented work, several dorsomorphin derivatives have been efficiently synthesized, based on a previously reported synthetic protocol with minor modifications. The endeavor was reinforced by a molecular docking study on the interactions of the designed derivatives with various protein targets, while the inhibitory effects of the synthesized novel molecules on the proliferation of murine leukemia cells (L1210), human T-lymphoc

SUBMITTER: Tzanetou EN 

PROVIDER: S-EPMC12839441 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature