Novel matrinic acid derivatives bearing 2‐anilinothiazole structure for non‐small cell lung cancer treatment with improved Hsp90 targeting effect

Involved in mediating the folding and maturation of more than 300 client proteins, many of which are oncoproteins, Hsp90 has emerged as a promising drug target for cancer therapy. In particular, inhibiting Hsp90 plays a vital role in the treatment of non‐small cell lung cancer. Owing to undesirable...

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Veröffentlicht in:Drug development research 2022-09, Vol.83 (6), p.1434-1454
Hauptverfasser: Xu, Yiming, Zeng, Panke, Wang, Haodong, Han, Keyan, Qiu, Gan, Wei, Yongquan, Chen, Rui, Wang, Lisheng, Liu, Xu
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Sprache:eng
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Zusammenfassung:Involved in mediating the folding and maturation of more than 300 client proteins, many of which are oncoproteins, Hsp90 has emerged as a promising drug target for cancer therapy. In particular, inhibiting Hsp90 plays a vital role in the treatment of non‐small cell lung cancer. Owing to undesirable outcomes of Hsp90 inhibitors in clinical trials, a series of matrinic acid compounds bearing 2‐anilinothiazole moiety were designed based on the structural features allocation shared among Hsp90 inhibitors within the ATP‐binding pocket. Most of the compounds showed potent anticancer activities validated by MTT assay. Among them, the most potent compound C4 (IC50 
ISSN:0272-4391
1098-2299
DOI:10.1002/ddr.21974