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

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.
* Authors to whom correspondence should be addressed.
Received: 30 September 2011; in revised form: 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

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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.

AMA 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(11):9178-9193.

Chicago/Turabian Style

Chen, Xiaofang; Wang, Li; Du, Yu; Wu, Yanbin; Jia, Xiaojian; Yang, Yuan; Hong, Bin. 2011. "Design, Synthesis and Biological Evaluation of Hydroxamic Acid Derivatives as Potential High Density Lipoprotein (HDL) Receptor CLA-1 Up-Regulating Agents." Molecules 16, no. 11: 9178-9193.

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