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Most compounds displayed weak moderate inhibition of DHDPS.
The biological characterization for the piperidinedione analogues revealed that most compounds displayed high inhibitory activity against APN.
Most compounds displayed good to excellent potency against four tested cancer cell lines as compared with GDC-0941 and sorafenib.
Most compounds displayed good to excellent potency against four tested cancer cell lines as compared with foretinib.
Most compounds displayed significantly improved activity against wild-type HIV-1 with EC50 values in single-digit nanomolar concentrations compared to etravirine VRX-480773 hybrids.
The biological screening results indicated that most compounds displayed potent inhibitory activity for Aβ (1 42) self-aggregation, and obvious selective inhibition to MAO-B.
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The most active compounds displayed sub-micromolar activities; compounds 56, 57, 58 and 63 were found to be the most active.
Two of most potent compounds displayed no apparent cytotoxicity toward MCF-10A normal mammary epithelial cells at 1 μM concentration.
Notably, most of compounds displayed remarkable tyrosinase inhibitory activities with IC50 value of lower than 1.0 μM.
Most synthesized compounds displayed good activity against human leukemia K562 cells in MTT tests, with compound 6d exhibiting the highest activity with IC50 value at 0.46 μM.
The biological screening results indicated that most of compounds displayed potent inhibitory activity for AChE and BuChE, and clearly selective inhibition to MAO-B.
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