C-dimethylated Chalcones:Towards Possible Dual Acting Agents-Against Tuberculosis and cancer(A549) and an SAR study

Abstract

A series of seventeen C-dimethyl chalcones on ring ‘A’ were synthesized by using a known condensation method. The chalcones include the utilization of heterocyclic aldehydes such as N,N-dimethyl benzaldehyde, furfural-2-aldehyde, and N-methyl indole aldehyde. All the compounds were found to possess moderate to potent anticancer activity on human lung adenocarcinoma cell line “A549” in the MTT cell proliferation method. The dimethyl chalcone 9f with furfural ring was found to possess potent anti-cancer activity followed by 9m with o-chloro substitution on ring ‘B’ with IC50values of 1.0 and 1.2 μg/mL respectively. Similarly compounds 9n, 9j, 9g, 9k, 9p, 9d, 9b,and 9ealso showed good anti-cancer activity (IC50values from 6.5 to 9.8μg/mL). Further, the compounds were also compared with the known anti-TB activities in order to ascertain their properties towards dual acting agents against tuberculosis and cancer for more beneficiaries.