Bioorganic and medicinal chemistry letters (2020)
Update date:2022-08-05
Topics: Inhibitors Novel Antitumor Activity Discovery Potent Activity Experimental
Hong, Soojung
Jeong, Jinah
Jung, Juyoung
Kim, Jeong-ah
Kwon, Jinsun
Kwon, Sungwook
Lee, Hongsub
Lee, Jeewoo
Lee, Jin Hee
Lee, Myoungjae
Moon, An-Na
A series of isosteric surrogates of the 4-phenyl group in luminespib were investigated as new scaffolds of the Hsp90 inhibitor for the discovery of novel antitumor agents. Among the synthesized surrogates of isoxazole and pyrazole, compounds 4a, 5e and 12b exhibited potent Hsp90 inhibition in ATPase activity and Her2 degradation assays and significant antitumor activity in A2780 and HCT116 cell lines. Animal studies indicated that compared to luminespib, their activities were superior in A2780 or NCI-H1975 tumor xenograft models. A molecular modeling study demonstrated that compound 4a could fit nicely into the N-terminal ATP binding pocket.
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