Literature DB >> 15056005

Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.

Stig Jönsson1, Gunnar Andersson, Tomas Fex, Tomas Fristedt, Gunnar Hedlund, Karl Jansson, Lisbeth Abramo, Ingela Fritzson, Olga Pekarski, Anna Runström, Helena Sandin, Ingela Thuvesson, Anders Björk.   

Abstract

Roquinimex-related 3-quinolinecarboxamide derivatives were prepared and evaluated for treatment of autoimmune disorders. The compounds were tested in mice for their inhibitory effects on disease development in the acute experimental autoimmune encephalomyelitis model and selected compounds in the beagle dog for induction of proinflammatory reaction. Structure-activity relationships are discussed. Compound 8c, laquinimod, showed improved potency and superior toxicological profile compared to the lead compound roquinimex (1b, Linomide) and was selected for clinical studies (currently in phase II).

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Year:  2004        PMID： 15056005     DOI： 10.1021/jm031044w

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  35 in total

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Authors:  Andrew P Robinson; Christopher T Harp; Avertano Noronha; Stephen D Miller
Journal:  Handb Clin Neurol       Date:  2014

Review 3.  The effects and side effects of laquinimod for the treatment of multiple sclerosis patients: a systematic review and meta-analysis of clinical trials.

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4.  Estrogen exacerbates mammary involution through neutrophil-dependent and -independent mechanism.

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Journal:  Elife       Date:  2020-07-24       Impact factor: 8.140

5.  Novel quinolinone-pyrazoline hybrids: synthesis and evaluation of antioxidant and lipoxygenase inhibitory activity.

Authors:  Ioanna Kostopoulou; Antonia Diassakou; Eleni Kavetsou; Eftichia Kritsi; Panagiotis Zoumpoulakis; Eleni Pontiki; Dimitra Hadjipavlou-Litina; Anastasia Detsi
Journal:  Mol Divers       Date:  2020-02-17       Impact factor: 2.943

6.  Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors.

Authors:  Anders Olsson; Anders Björk; Johan Vallon-Christersson; John T Isaacs; Tomas Leanderson
Journal:  Mol Cancer       Date:  2010-05-17       Impact factor: 27.401

7.  Risks vs benefits of glatiramer acetate: a changing perspective as new therapies emerge for multiple sclerosis.

Authors:  Kenneth P Johnson
Journal:  Ther Clin Risk Manag       Date:  2010-04-15       Impact factor: 2.423

Review 8.  Small molecules in the treatment of systemic lupus erythematosus.

Authors:  Anastasia Markopoulou; Vasileios C Kyttaris
Journal:  Clin Immunol       Date:  2012-10-02       Impact factor: 3.969

Review 9.  Benefits versus risks of latest therapies in multiple sclerosis: a perspective review.

Authors:  Daniel Ontaneda; Daniela Di Capua
Journal:  Ther Adv Drug Saf       Date:  2012-12

10.  Open-label, clinical phase I studies of tasquinimod in patients with castration-resistant prostate cancer.

Authors:  O Bratt; M Häggman; G Ahlgren; O Nordle; A Björk; J-E Damber
Journal:  Br J Cancer       Date:  2009-09-15       Impact factor: 7.640
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