Literature DB >> 17317170

Optimization of halopemide for phospholipase D2 inhibition.

Lauren Monovich1, Benjamin Mugrage, Elizabeth Quadros, Karen Toscano, Ruben Tommasi, Stacey LaVoie, Eugene Liu, Zhengming Du, Daniel LaSala, William Boyar, Paul Steed.   

Abstract

Halopemide, which was identified by HTS to inhibit phospholipase D2 (PLD2), provided the basis for an exploratory effort to identify potent inhibitors of PLD2 for use as inflammatory mediators. Parallel synthesis and purification were utilized to rapidly identify orally available amide analogs derived from indole 2-carboxylic acids with superior potency versus PLD2.

Entities:  

Mesh：

Substances：

Year:  2007        PMID： 17317170     DOI： 10.1016/j.bmcl.2007.01.059

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  52 in total

1.  Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor.

Authors:  Robert R Lavieri; Sarah A Scott; Paige E Selvy; Kwangho Kim; Satyawan Jadhav; Ryan D Morrison; J Scott Daniels; H Alex Brown; Craig W Lindsley
Journal:  J Med Chem       Date:  2010-09-23       Impact factor: 7.446

2.  The Role of Phospholipase D in Regulated Exocytosis.

Authors:  Tatiana P Rogasevskaia; Jens R Coorssen
Journal:  J Biol Chem       Date:  2015-10-02       Impact factor: 5.157

Review 3.  The interface between phosphatidylinositol transfer protein function and phosphoinositide signaling in higher eukaryotes.

Authors:  Aby Grabon; Vytas A Bankaitis; Mark I McDermott
Journal:  J Lipid Res       Date:  2018-11-30       Impact factor: 5.922

Review 4.  Phosphatidic acid signaling to mTOR: signals for the survival of human cancer cells.

Authors:  David A Foster
Journal:  Biochim Biophys Acta       Date:  2009-03-02

Review 5.  Phospholipase D: enzymology, functionality, and chemical modulation.

Authors:  Paige E Selvy; Robert R Lavieri; Craig W Lindsley; H Alex Brown
Journal:  Chem Rev       Date:  2011-09-22       Impact factor: 60.622

6.  Discovery of compounds blocking the proliferation of Toxoplasma gondii and Plasmodium falciparum in a chemical space based on piperidinyl-benzimidazolone analogs.

Authors:  Nadia Saïdani; Cyrille Y Botté; Michael Deligny; Anne-Laure Bonneau; Janette Reader; Ronald Lasselin; Goulven Merer; Alisson Niepceron; Fabien Brossier; Jean-Christophe Cintrat; Bernard Rousseau; Lyn-Marie Birkholtz; Marie-France Cesbron-Delauw; Jean-François Dubremetz; Corinne Mercier; Henri Vial; Roman Lopez; Eric Maréchal
Journal:  Antimicrob Agents Chemother       Date:  2014-02-18       Impact factor: 5.191

7.  Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.

Authors:  Robert Lavieri; Sarah A Scott; Jana A Lewis; Paige E Selvy; Michelle D Armstrong; H Alex Brown; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-03-06       Impact factor: 2.823

Review 8.  Targeting phospholipase D with small-molecule inhibitors as a potential therapeutic approach for cancer metastasis.

Authors:  Wenjuan Su; Qin Chen; Michael A Frohman
Journal:  Future Oncol       Date:  2009-11       Impact factor: 3.404

9.  Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.

Authors:  Matthew C O'Reilly; Sarah A Scott; Kyle A Brown; Thomas H Oguin; Paul G Thomas; J Scott Daniels; Ryan Morrison; H Alex Brown; Craig W Lindsley
Journal:  J Med Chem       Date:  2013-03-13       Impact factor: 7.446

Review 10.  Functional regulation of phospholipase D expression in cancer and inflammation.

Authors:  Dong Woo Kang; Kang-Yell Choi; Do Sik Min
Journal:  J Biol Chem       Date:  2014-07-02       Impact factor: 5.157
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.