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Molecules 2011, 16(11), 9178-9193; doi:10.3390/molecules16119178

Design, Synthesis and Biological Evaluation of Hydroxamic Acid Derivatives as Potential High Density Lipoprotein (HDL) Receptor CLA-1 Up-Regulating Agents

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
These authors contributed equally to this work.
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Received: 30 September 2011 / Revised: 20 October 2011 / Accepted: 28 October 2011 / Published: 2 November 2011
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Abstract

Trichostatin A (TSA) and suberoylanilide hydroxamic acid (SAHA) were reported in our recent publication as novel human high density lipoprotein (HDL) receptor CD36 and Lysosomal integral membrane protein-II Analogous-1 (CLA-1) up-regulators. As part of a broader effort to more fully explore the structure-activity relationships (SAR) of CLA-1 up-regulators, we synthesized a series of hydroxamic acid derivatives and evaluated their CLA-1 up-regulating activities in HepG2 cells. Some compounds exhibited over 10-fold up-regulation of CLA-1 expression in HepG2 cells at 10 μg/mL concentration. The compound 1g showed the best potency, with a lower EC50 than TSA (EC50 = 0.32 μM versus 1.2 μM). These compounds provide early new CLA-1 up-regulators with potential for treating atherosclerosis.
Keywords: high density lipoprotein receptor; up-regulator; CLA-1; trichostatin A (TSA); suberoylanilide hydroxamic acid (SAHA); hydroxamic acid high density lipoprotein receptor; up-regulator; CLA-1; trichostatin A (TSA); suberoylanilide hydroxamic acid (SAHA); hydroxamic acid
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Chen, X.; Wang, L.; Du, Y.; Wu, Y.; Jia, X.; Yang, Y.; Hong, B. Design, Synthesis and Biological Evaluation of Hydroxamic Acid Derivatives as Potential High Density Lipoprotein (HDL) Receptor CLA-1 Up-Regulating Agents. Molecules 2011, 16, 9178-9193.

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