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Lead optimization of HMBA to develop potent HEXIM1 inducers

B Zhong, R Lama, W Ketchart, MM Montano…

文献索引:Zhong, Bo; Lama, Rati; Ketchart, Wannarasmi; Montano, Monica M.; Su, Bin Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 5 p. 1410 - 1413

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被引用次数: 5

摘要

Abstract The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives inducing Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in LNCaP prostate cancer cells. Several compounds with unsymmetrical structures showed significantly improved activity. Distinct from HMBA, these analogs have increased hydrophobicity and can improve the short half-life of HMBA, which is one of the factors that ...