Literature DB >> 14684297

Discovery of a novel series of DHODH inhibitors by a docking procedure and QSAR refinement.

Johann Leban1, Wael Saeb, Gabriel Garcia, Roland Baumgartner, Bernd Kramer.   

Abstract

A novel series of DHODH inhibitors was developed based on a lead which was obtained by a docking procedure and a medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method to yield low nanomolar inhibitors.

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Year:  2004        PMID： 14684297     DOI： 10.1016/j.bmcl.2003.10.021

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


  6 in total

1.  3D-QSAR studies on a series of dihydroorotate dehydrogenase inhibitors: analogues of the active metabolite of leflunomide.

Authors:  Shun-Lai Li; Mao-Yu He; Hong-Guang Du
Journal:  Int J Mol Sci       Date:  2011-05-10       Impact factor: 5.923

2.  Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH).

Authors:  Marianne Lucas-Hourani; Hélène Munier-Lehmann; Farah El Mazouni; Nicholas A Malmquist; Jane Harpon; Eloi P Coutant; Sandrine Guillou; Olivier Helynck; Anne Noel; Artur Scherf; Margaret A Phillips; Frédéric Tangy; Pierre-Olivier Vidalain; Yves L Janin
Journal:  J Med Chem       Date:  2015-06-30       Impact factor: 7.446

3.  Development of a human dihydroorotate dehydrogenase (hDHODH) pharma-similarity index approach with scaffold-hopping strategy for the design of novel potential inhibitors.

Authors:  Kuei-Chung Shih; Chi-Ching Lee; Chi-Neu Tsai; Yu-Shan Lin; Chuan-Yi Tang
Journal:  PLoS One       Date:  2014-02-04       Impact factor: 3.240

4.  On the interactions of leflunomide and teriflunomide within receptor cavity--NMR studies and energy calculations.

Authors:  Jacek Kujawski; Marek K Bernard; Elżbieta Jodłowska; Kornelia Czaja; Beata Drabińska
Journal:  J Mol Model       Date:  2015-04-08       Impact factor: 1.810

5.  UVB-induced DHODH upregulation, which is driven by STAT3, is a promising target for chemoprevention and combination therapy of photocarcinogenesis.

Authors:  Mohsen Hosseini; Léa Dousset; Pauline Michon; Walid Mahfouf; Elodie Muzotte; Vanessa Bergeron; Doriane Bortolotto; Rodrigue Rossignol; François Moisan; Alain Taieb; Anne-Karine Bouzier-Sore; Hamid R Rezvani
Journal:  Oncogenesis       Date:  2019-09-24       Impact factor: 7.485

6.  Store-Operated Calcium Entry as a Therapeutic Target in Acute Pancreatitis: Discovery and Development of Drug-Like SOCE Inhibitors.

Authors:  Marta Serafini; Celia Cordero-Sanchez; Rosanna Di Paola; Irene P Bhela; Silvio Aprile; Beatrice Purghè; Roberta Fusco; Salvatore Cuzzocrea; Armando A Genazzani; Beatrice Riva; Tracey Pirali
Journal:  J Med Chem       Date:  2020-11-30       Impact factor: 7.446
  6 in total

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