Abstract
A series of 1, 3-diaryl-2-propen-1-ones was synthesised in order to obtain a new type of anticancer drug, designed with hybrid features to inhibit colon cancer activated receptor. Based on computational modelling and docking studies, potential inhibitors were synthesised and their biological activity evaluated. The structures of newly synthesized compounds were confirmed by 1 HNMR, 13 CNMR and Mass spectrometry. All analogues were evaluated for in vitro cytotoxicity against human colon (caco-2) cancer cell lines. Compounds 1b, 1f-1h, and 2i showed significant cytotoxicity. Chalcones 1b, 1f and 1g were identified as the most potent and selective anticancer agents with IC 50 values <1 µg/mL and 1.5 µg/mL, against caco-2 cell line, respectively. In conclusion, this finding confirms the suitability of indolyl chalcone analogues as candidates for further investigation towards the management of colon cancer related diseases.
Highlights
Various research groups have focused on chemoprevention and working on development of new lead molecules
Chalcones are 1,3-diaryl-2-propen-1ones in which two aromatic rings are joined by a three carbon bridge having a carbonyl moiety and, unsaturation (Aggarwal et al, 2005)
In this study both series of indolyl chalcones found in good yields, which are in line with aforementioned references
Summary
Various research groups have focused on chemoprevention and working on development of new lead molecules.
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