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Design, synthesis and structure-activity relationship of phthalimides endowed with dual antiproliferative and immunomodulatory activities.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2015; Vol. 96, pp. 491-503. Date of Electronic Publication: 2015 Apr 20. - Publication Year :
- 2015
-
Abstract
- The present work reports the synthesis and evaluation of the antitumour and immunomodulatory properties of new phthalimides derivatives designed to explore molecular hybridization and bioisosterism approaches between thalidomide, thiosemicarbazone, thiazolidinone and thiazole series. Twenty-seven new molecules were assessed for their immunosuppressive effect toward TNFα, IFNγ, IL-2 and IL-6 production and antiproliferative activity. The best activity profile was observed for the (6a-f) series, which presents phthalyl and thiazolidinone groups.<br /> (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Animals
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Proliferation drug effects
Cells, Cultured
Crystallography, X-Ray
Cytokines analysis
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Lymphocytes drug effects
Macrophages drug effects
Male
Mice
Mice, Inbred BALB C
Models, Molecular
Molecular Structure
Phthalimides chemical synthesis
Phthalimides chemistry
Structure-Activity Relationship
Antineoplastic Agents pharmacology
Drug Design
Immunomodulation
Phthalimides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 96
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 25942060
- Full Text :
- https://doi.org/10.1016/j.ejmech.2015.04.041