2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors - PubMed (original) (raw)

. 2007 Jun 1;17(11):3208-11.

doi: 10.1016/j.bmcl.2007.03.017. Epub 2007 Mar 12.

Haixia Wang, Joseph A Tino, Jeffrey A Robl, Timothy F Herpin, R Michael Lawrence, Scott Biller, Haris Jamil, Randy Ponticiello, Luping Chen, Ching-hsuen Chu, Neil Flynn, Dong Cheng, Rulin Zhao, Bangchi Chen, Dora Schnur, Mary T Obermeier, Vito Sasseville, Ramesh Padmanabha, Kristen Pike, Thomas Harrity

Affiliations

• PMID: 17383874
• DOI: 10.1016/j.bmcl.2007.03.017

2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors

James J Li et al. Bioorg Med Chem Lett. 2007.

Abstract

A novel series of 2-hydroxy-N-arylbenzenesulfonamides were identified to be ATP-citrate lyase (ACL) inhibitors with compound 9 displaying potent in vitro activity (IC(50)=0.13 microM). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma cholesterol, triglyceride, and glucose, as well as inhibited weight gain.

PubMed Disclaimer

Similar articles

• ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R,5S)-omega-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo.
  Gribble AD, Ife RJ, Shaw A, McNair D, Novelli CE, Bakewell S, Shah VP, Dolle RE, Groot PH, Pearce N, Yates J, Tew D, Boyd H, Ashman S, Eggleston DS, Haltiwanger RC, Okafo G. Gribble AD, et al. J Med Chem. 1998 Sep 10;41(19):3582-95. doi: 10.1021/jm980091z. J Med Chem. 1998. PMID: 9733484
• ATP-citrate lyase as a target for hypolipidemic intervention. Design and synthesis of 2-substituted butanedioic acids as novel, potent inhibitors of the enzyme.
  Gribble AD, Dolle RE, Shaw A, McNair D, Novelli R, Novelli CE, Slingsby BP, Shah VP, Tew D, Saxty BA, Allen M, Groot PH, Pearce N, Yates J. Gribble AD, et al. J Med Chem. 1996 Aug 30;39(18):3569-84. doi: 10.1021/jm960167w. J Med Chem. 1996. PMID: 8784456
• Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs.
  Shrestha S, Bhattarai BR, Lee KH, Cho H. Shrestha S, et al. Bioorg Med Chem. 2007 Oct 15;15(20):6535-48. doi: 10.1016/j.bmc.2007.07.010. Epub 2007 Jul 26. Bioorg Med Chem. 2007. PMID: 17692525
• ATP citrate lyase inhibitors as novel cancer therapeutic agents.
  Zu XY, Zhang QH, Liu JH, Cao RX, Zhong J, Yi GH, Quan ZH, Pizzorno G. Zu XY, et al. Recent Pat Anticancer Drug Discov. 2012 May 1;7(2):154-67. doi: 10.2174/157489212799972954. Recent Pat Anticancer Drug Discov. 2012. PMID: 22339355 Review.
• ATP-citrate lyase: genetics, molecular biology and therapeutic target for dyslipidemia.
  Burke AC, Huff MW. Burke AC, et al. Curr Opin Lipidol. 2017 Apr;28(2):193-200. doi: 10.1097/MOL.0000000000000390. Curr Opin Lipidol. 2017. PMID: 28059952 Review.

Cited by

• Discovery of Flavonoids as Novel Inhibitors of ATP Citrate Lyase: Structure-Activity Relationship and Inhibition Profiles.
  Wang P, Hou T, Xu F, Luo F, Zhou H, Liu F, Xie X, Liu Y, Wang J, Guo Z, Liang X. Wang P, et al. Int J Mol Sci. 2022 Sep 15;23(18):10747. doi: 10.3390/ijms231810747. Int J Mol Sci. 2022. PMID: 36142671 Free PMC article.
• Emerging roles of the chromatin remodeler MORC2 in cancer metabolism.
  Mohapatra B, Pakala SB. Mohapatra B, et al. Med Oncol. 2024 Aug 8;41(9):221. doi: 10.1007/s12032-024-02464-9. Med Oncol. 2024. PMID: 39117768 Review.
• ATP citrate lyase mediates resistance of colorectal cancer cells to SN38.
  Zhou Y, Bollu LR, Tozzi F, Ye X, Bhattacharya R, Gao G, Dupre E, Xia L, Lu J, Fan F, Bellister S, Ellis LM, Weihua Z. Zhou Y, et al. Mol Cancer Ther. 2013 Dec;12(12):2782-91. doi: 10.1158/1535-7163.MCT-13-0098. Epub 2013 Oct 16. Mol Cancer Ther. 2013. PMID: 24132143 Free PMC article.
• A novel direct homogeneous assay for ATP citrate lyase.
  Ma Z, Chu CH, Cheng D. Ma Z, et al. J Lipid Res. 2009 Oct;50(10):2131-5. doi: 10.1194/jlr.D900008-JLR200. Epub 2009 Mar 12. J Lipid Res. 2009. PMID: 19286649 Free PMC article.
• Effect of Food Additive Citric Acid on The Growth of Human Esophageal Carcinoma Cell Line EC109.
  Chen X, Lv Q, Liu Y, Deng W. Chen X, et al. Cell J. 2017 Winter;18(4):493-502. doi: 10.22074/cellj.2016.4716. Epub 2016 Sep 26. Cell J. 2017. PMID: 28042534 Free PMC article.

MeSH terms

Substances

LinkOut - more resources

• Full Text Sources

  • Elsevier Science

• Other Literature Sources

  • The Lens - Patent Citations Database

• Chemical Information

  • BindingDB

• Molecular Biology Databases

  • Guide to Pharmacology