Anti-metastatic propensity of biscoumarin scaffold synthesized under catalyst free aqueous phase microwave irradiation

Abstract

An environmentally benign, catalyst free, aqueous phase, microwave assisted method for the synthesis of biscoumarin derivatives using 4-hydroxycoumarin and different aldehydes is reported. The comparative investigation of the same synthetic methodology under conventional refluxing, domestic and scientific programmable microwave synthesizer has been attempted for the purpose of comparing the reaction performance in terms of % yield, reaction time, reproducibility and reaction control. In addition to the increased yields and attenuated reaction times for biscoumarin synthesis, the difficulty of reaction control and result reproducibility usually encountered with domestic microwave ovens have been addressed through an optimized synthetic methodology using microwave synthesizer. Screening bioactive compounds for their propensity towards inhibition of cancer metastasis is a must step in advancement of cancer chemotherapy. The synthesized biscoumarin scaffold was investigated for inhibitory metastatic activity against human lung carcinoma cell line, A549 through in vitro wound healing and invasion assays. The biscoumarin scaffold was found to possess an effective anti-proliferative activity. It was also found to be efficient in ablating the migration and invasiveness of these cells under in vitro conditions.