Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents
C Tacon, EM Guantai, PJ Smith, K Chibale
Index: Tacon, Claire; Guantai, Eric M.; Smith, Peter J.; Chibale, Kelly Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 2 p. 893 - 902
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Citation Number: 11
Abstract
Herein we report on the semisynthesis and biological evaluation of β-amino alcohol derivatives of the natural product totarol and other simple aromatic systems. All β-amino alcohol derivatives of totarol exhibited higher antiplasmodial activity than totarol [IC50: 11.69 μM (K1, chloroquine and multi-drug resistant strain), and 11.78 μM (D10, chloroquine sensitive strain)]—12e was the most active [IC50: 0.63 μM (K1), and 0.61 μM (D10)]. The ...
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