Design and synthesis of Hsp90 inhibitors: exploring the SAR of Sansalvamide A derivatives

…, LD Alexander, VA Johnson, CC Lin, J Savage…

文献索引：Sellers, Robert P.; Alexander, Leslie D.; Johnson, Victoria A.; Lin, Chun-Chieh; Savage, Jeremiah; Corral, Ricardo; Moss, Jason; Slugocki, Tim S.; Singh, Erinprit K.; Davis, Melinda R.; Ravula, Suchitra; Spicer, Jamie E.; Oelrich, Jenna L.; Thornquist, Andrea; Pan, Chung-Mao; McAlpine, Shelli R. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 18 p. 6822 - 6856

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被引用次数: 58

摘要

Utilizing the structure–activity relationship we have developed during the synthesis of the first two generations and mechanism of action studies that point to the interaction of these molecules with the key oncogenic protein Hsp90, we report here the design of 32 new Sansalvamide A derivatives and their synthesis. Our new structures, designed from previously reported potent compounds, were tested for cytotoxicity on the HCT116 colon ...