Discovery of hybrid Hsp90 inhibitors and their anti-neoplastic effects against gefitinib-resistant non-small cell lung cancer (NSCLC)

CH Jeong, HB Park, WJ Jang, SH Jung…

Index: Jeong, Chul-Ho; Park, Hee Baek; Jang, Won Jun; Jung, Su Hyun; Seo, Young Ho Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 1 p. 224 - 227

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Citation Number: 7

Abstract

Abstract Heat shock protein 90 (Hsp90) represents an attractive cancer therapeutic target due to its role in the stabilization and maturation of many oncogenic proteins. We have designed a series of hybrid Hsp90 inhibitors by connecting the resorcinol ring of VER-49009 (2) and the trimethoxyphenyl ring of PU3 (3) using structure-based approach. Subsequent testing established that compound 1f inhibited gefitinib-resistant H1975 cell proliferation, ...