Objective: Colorectal cancer (CRC) is the third most frequently occurring cancer in both male and females, but it ranks second in developed countries. The incidence of colorectal cancer is still increasing in large parts of the world due to the development of resistance to the available drugs. Thus, there is a need to develop novel colorectal anti cancer agents. Materials and Methods: The present work includes the synthesis of a series of new 7-(Substituted benzylidene)-3-aryl-2,3,4,5,6,7-hexahydroindazol-1-yl(pyridine-4-yl)methanones from substituted chalcones. These chalcones were prepared by Claisen-Schmidt reaction by the condensation of cyclohexanone and various substituted aromatic aldehydes. The synthesized compounds were confirmed by IR, 1H NMR, MASS spectra and CHNO Elemental analysis. The synthesized compounds were predicted for biological activities by Insilico method based on those predictions the compounds screened for colorectal anti cancer activity (MTT assay) by using cell line HT-29 human colorectal adenocarcinoma using cisplatin as standard drug. Results: The compounds 2a, 2c, 2f, 3a, 3c and 3f exhibited maximum activity at a concentration <10 �µg, 2b, 2e, 3b and 3e exhibited moderate activity at a concentration <20 �µg. Remaining compounds 2d and 3d exhibited no activity at concentration >30 �µg. Conclusion: The synthesized compounds having the electron releasing groups such as hydroxyl and dimethyl amino group in phenyl ring exhibited maximum activity. Hence it clearly indicates the importance of electron releasing groups on aromatic rings for anticancer activity.
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