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In CAM assay, compound 24c and 30c presented significantly anti-angiogenesis activity comparable with 2-methoxyestradiol.
In ABTS free radicals scavenging assay compound 1 exhibited 88.51 ± 0.62 % inhibition at highest tested concentration i.e., 1000 μg/mL.
In cell-based cartilage explants assay compound 48produced87%7% inhibition of proteoglycan degradation at 10 μg/mL.
By the modified TRAP assay, compound 13i exhibited the most potent inhibitory activity against telomerase with an IC50 value of 0.98 μM.
When tested in a replicon assay, compound 2h was the sole derivative to also display anti-HCV activity (EC50 = 3.1 μM).
Interestingly, the most potent compound in MTT assay, compound 12b, exhibited high inhibitory activity against COX-2 with selectivity index (COX-1/COX-2) > 100.
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In the FS-3 assay, compounds 20 and 21 significantly inhibited the ATX at low nanomolar level (IC50 = 2.99 and 2.19 nM, respectively).
Based on the outcome of in vitro COX assay, compounds 3c 3e and 4c 4e (IC50 0.60–1.11 μM) elicited an interesting profile as competitive selective COX-2 inhibitors.
In Topoisomerase I (Topo I -induced DNA cleavage assay, compounds 6a, 6d, and 6k, as compared to CPT, revealed hI -induced I inhibitory activity.
In the VDR competitive binding assay, compounds 2 and 3 almost lost their binding ability, and were only 0.01% and 0.015% as potent as the 1α,25-dihydroxyvitamin D3.
In the AChE inhibition assay, compounds 1, 2, 4, 5, 7 9, and 11 13 showed the moderate activity on the inhibition of AChE with the IC50 values ranging from 54.4 to 94.6 μM, compared with berberine (IC50o of 0.67 μM).
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