Phenanthridine Derivatives as Promising New Anticancer Agents: synthesis, Biological Evaluation and Binding Studies

Abstract

<b>Aim:</b> Phenanthridines are an essential class of nitrogenous heterocycles with extensive applications in medicinal chemistry. The development of efficient and eco-friendly methods for the preparation of chirally pure dihydropyrrolo[1,2-<i>f</i>]phenanthridines (<b>5a-h</b>), and their <i>in vitro</i> evaluation and modeling studies as potential anticancer, antioxidant and DNA cleavage agents is reported. <b>Methodology & results:</b> Compounds <b>5a-h</b> were prepared through a facile one-pot synthesis and characterized by infrared, high resolution mass spectrometry, ¹H and ¹³C nuclear magnetic resonance. The molecules were subjected to virtual screening and docking analysis against selected human molecular targets. Compound <b>5g</b> displayed good binding properties as well as significant anticancer and DNA cleavage activity. <b>Conclusion:</b> Compound <b>5g</b> has been identified as a potential lead candidate for further testing against additional cancer cell lines and animal models in future.