Journal
FUTURE MEDICINAL CHEMISTRY
Volume 12, Issue 8, Pages 709-739Publisher
Newlands Press Ltd
DOI: 10.4155/fmc-2019-0016
Keywords
anticancer; antioxidant; DNA cleavage; docking; molecular screening; synthesis
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Funding
- Government of India agency, Department of Biotechnology
- Government of India agency, Indian Council of Medical Research
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Aim: 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-f]phenanthridines (5a-h), and their in vitro evaluation and modeling studies as potential anticancer, antioxidant and DNA cleavage agents is reported. Methodology & results: Compounds 5a-h were prepared through a facile one-pot synthesis and characterized by infrared, high resolution mass spectrometry, H-1 and C-13 nuclear magnetic resonance. The molecules were subjected to virtual screening and docking analysis against selected human molecular targets. Compound 5g displayed good binding properties as well as significant anticancer and DNA cleavage activity. Conclusion: Compound 5g has been identified as a potential lead candidate for further testing against additional cancer cell lines and animal models in future. Graphical abstract
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