Novel synthesised chrysin derivatives offer noteworthy insight into the structural scaffolds required for improved anti-proliferative activity

Abstract

In the present investigations, a novel series of chrysin derivatives were prepared using Mannich base approach and screened for in vitro antiproliferative activity against human cancer cells. Among the derivatives, 4e exhibited 10 fold improved anti-proliferative efficiency than the free chrysin. The correlation of chemical structural core–biological efficiency indicated that free hydroxyl groups and the substituents in the B-ring were involved in the improved anti-proliferative efficiencies. The removal of oxygen atom in the ring C by the utilization of different aliphatic/aromatic/heterocyclic molecules to arrive different structural motifs could lead to chrysin derivatives with desirable structural features were also increased lipophilic character and stability in medium. The prepared compounds exhibited strong antiproliferative efficacies may be mimics the natural flavone derivatives. The utmost promising structural lead molecules in particular the chrysin derivatives 4e, 4f and 4 g, will be screened for their anti-proliferative activities against a broader range of cancer cell lines (obtained from cancer Institute) and may be potent molecule for anticancer agents. The synthesized chrysin derivatives have obeyed Lipinski’s “rule of five” and have drug-likeness.