1330740-56-1Relevant articles and documents
Discovery of novel heat shock protein (Hsp90) inhibitors based on luminespib with potent antitumor activity
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
, (2020/04/27)
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.
A NOVEL 5-MEMBERED HETEROCYCLE DERIVATIVES AND MANUFACTURING PROCESS THEREOF
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Page/Page column 115-116, (2011/09/19)
Disclosed herein are a novel 5-membered heterocycle derivatives represented by Formula I, a tautomer, pharmaceutically approved salts thereof, prodrug of this compound, or pharmaceutically use. Accordingly this prevent invention, a novel 5-membered heterocycle derivatives, a tautomer, pharmaceutically approved salt, or prodrug show antitumoral activity. Thus, this compounds are useful in the treatment of tumor.
