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However it is also apparent that there was essentially no selectivity over the human MRC5 cells, with most compounds showing a ratio of EC50 (MRC5)/EC50 (T. brucei) of ⩽3.
Most compounds showing inhibition of MurG contained a 2-methoxyphenyl R1 substituent, whilst no compound containing a phenyl R1 substituent inhibited MurG, consistent with a favourable hydrogen-bonding interaction between the 2-methoxy substituent and the MurG active site.
The micronucleus assay supported these findings with most compounds showing genotoxic properties due to the numbers of micronuclei (chromosomal aberrations) formed within the cultured mouse lymphoma cells (L5178Y), in comparison to controls.
Similar(57)
Most compounds showed moderate to excellent activity.
Most compounds showed potent HDAC6 inhibition activity.
Most compounds showed moderate to excellent potency.
Most compounds showed moderate-to-excellent antiproliferative activity.
Most compounds showed moderate to excellent antitumor activity.
Most compounds showed significant peripheral and/or central analgesic activity.
Most compounds showed weak to excellent antiproliferative activity.
Most compounds showed moderate to excellent inhibitory activities.
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