Design, synthesis, and docking of highly hypolipidemic agents: Schizosaccharomyces pombe as a new model for evaluating α-asarone-based HMG-CoA reductase …

…, L Villa-Tanaca, L Garduño-Siciliano, F Jiménez…

Index: Argueelles, Nancy; Sanchez-Sandoval, Eugenia; Mendieta, Aaron; Villa-Tanaca, Lourdes; Garduno-Siciliano, Leticia; Jimenez, Fabiola; Cruz, Maria del Carmen; Medina-Franco, Jose L.; Chamorro-Cevallos, German; Tamariz, Joaquin Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 12 p. 4238 - 4248

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Citation Number: 17

Abstract

A series of α-asarone-based analogues was designed by conducting docking experiments with published crystal structures of human HMG-CoA reductase. Indeed, synthesis and evaluation of this series showed a highly hypocholesterolemic in vivo activity in a murine model, as predicted by previous docking studies. In agreement with this model, the polar groups attached to the benzene ring could play a key role in the enzyme binding and ...