Design, synthesis and evaluation of aurone and indanone derivatives as novel antitumor agents.

An aurone derivative HJ-1, was isolated from Coreopsis tinctoria in our previous work, showed potential anti-hepatocellular carcinoma activity. From it, seventy-five compounds were synthesized via bioisostere and scaffold hopping strategy, and then submitted to the inhibitory activities evaluation against four tumor cells (HELA, HT-29, A549 and HepG2) through MTT assays. These activities have been discussed in SAR. Based on the results, compounds, thirty compounds showed moderate to good antitumour activity. Among them, five compounds (A3: 3.41 ± 1.03 μM, E3: 5.11 ± 0.23 μM, E8: 4.14 ± 1.21 μM, F2: 5.40 ± 1.18 μM, F4: 7.37 ± 0.87 μM) had achieved a comparable efficiency to the positive control DOX (Doxorubicin) against HT-29 cell lines, Compound A3 and F4 were identified as potential leading compounds. [ABSTRACT FROM AUTHOR]