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Fig. 5 Structure-activity relationship summary for on-target activity and antiproliferative activity in cancer cells. 3,4-Dichloro-5-methylpyrrolamide (in blue) moiety is critical for dual-target inhibition, while its replacement with the 3,4-dichlorobenzamide (in blue) moiety results in selective Hsp90 CTD inhibition. Introduction of the methoxy group on the adjacent phenyl ring (in yellow) results in equipotent activity, while modification of the nitrogen-based heterocycle (in magenta) results in the most pronounced effects on target inhibition and antiproliferative activity.
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