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Synthesis and biological activity of tetracyclic imidazo[4,5-b]pyridines

Due to the structural similarity of imidazo-pyridine heterocyclic system with naturally occurring purines and great therapeutic potential and significance in the drug discoivery. Imidazo[4, 5-b]pyridine scaffold is among the most privileged and important building blocks in organic and medicinal chemistry. [1, 2] In this work, we have synthesized novel amino substituted tetracyclic derivatives by using conventional and microwave assisted organic synthesis. The antiproliferative activity was studied against human cancer and non-tumour cells and the majority of compounds showed improvement of activity on HCT116 and MCF-7 cancer cells when compared to etoposide. oOtained results revealed that the position of N nitrogen in pyridine ring has strong impact on the biological activity. Thus, regioisomers 6, 30 and 32 showed noticeable enhancement of activity in comparison to their counterparts 10, 37 and 25 having IC50 values. Additionally, their interaction with ct-DNA was studied by several spectroscopic methods.

amines ; antiproliferative activity ; ct-DNA ; imidazo[4, 5-b]pyridines

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