1. Design, synthesis and structure-activity relationship of phthalimides endowed with dual antiproliferative and immunomodulatory activities.
- Author
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Cardoso MV, Moreira DR, Oliveira Filho GB, Cavalcanti SM, Coelho LC, Espíndola JW, Gonzalez LR, Rabello MM, Hernandes MZ, Ferreira PM, Pessoa C, Alberto de Simone C, Guimarães ET, Soares MB, and Leite AC
- 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
- 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., (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)
- Published
- 2015
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