1. Design, synthesis and structure–activity relationship of phthalimides endowed with dual antiproliferative and immunomodulatory activities.
- Author
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Cardoso, Marcos Veríssimo de Oliveira, Moreira, Diogo Rodrigo Magalhães, Filho, Gevanio Bezerra Oliveira, Cavalcanti, Suellen Melo Tiburcio, Coelho, Lucas Cunha Duarte, Espíndola, José Wanderlan Pontes, Gonzalez, Laura Rubio, Rabello, Marcelo Montenegro, Hernandes, Marcelo Zaldini, Ferreira, Paulo Michel Pinheiro, Pessoa, Cláudia, Alberto de Simone, Carlos, Guimarães, Elisalva Teixeira, Soares, Milena Botelho Pereira, and Leite, Ana Cristina Lima
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PHTHALIMIDES , *STRUCTURE-activity relationship in pharmacology , *ANTINEOPLASTIC agents , *IMMUNOLOGICAL adjuvants , *DRUG design , *CHEMICAL synthesis - 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. [ABSTRACT FROM AUTHOR]
- Published
- 2015
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