- A direct approach to orthogonally protected α-amino aldehydes
-
O-Neopentyl-xanthate 19 bearing a masked α-amino aldehyde, with the two functional groups orthogonally protected, reacts cleanly with many functional alkenes. The radical addition-transfer furnishes densely functionalized adducts that can be further transformed into an array of amino-substituted carbocycles and heteroaromatics. They are also easily converted into imidazolones.
- Lamb, Richard,Revil-Baudard, Vincent L.,Zard, Samir Z.
-
-
Read Online
- Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi
-
Chagas disease is a parasitic infection caused by protozoan Trypanosoma cruzi that affects approximately 6-7 million people worldwide. Benznidazole is the only drug approved for treatment during the acute and asymptomatic chronic phases; however, its efficacy during the symptomatic chronic phase is controversial. The present work reports the synthesis and anti-T. cruzi activities of a novel series of phthalimido-thiazoles. Some of these compounds showed potent inhibition of the trypomastigote form of the parasite at low cytotoxicity concentrations in spleen cells, and the resulting structure-activity relationships are discussed. We also showed that phthalimido-thiazoles induced ultrastructural alterations on morphology, flagellum shortening, chromatin condensation, mitochondria swelling, reservosomes alterations and endoplasmic reticulum dilation. Together, these data revealed, for the first time, a novel series of phthalimido-thiazoles-structure-based compounds with potential effects against T. cruzi and lead-like characteristics against Chagas disease.
- De Moraes Gomes, Paulo André Teixeira,Oliveira, Arsênio Rodrigues,De Oliveira Cardoso, Marcos Veríssimo,De Farias Santiago, Edna,De Oliveira Barbosa, Miria,De Siqueira, Lucianna Rabelo Pessoa,Moreira, Diogo Rodrigo Magalh?es,Bastos, Tanira Matutino,Brayner, Fábio André,Soares, Milena Botelho Pereira,De Oliveira Mendes, Andresa Pereira,De Castro, Maria Carolina Accioly Brelaz,Pereira, Valéria Rego Alves,Leite, Ana Cristina Lima
-
-
- Design, synthesis and structure - Activity relationship of phthalimides endowed with dual antiproliferative and immunomodulatory activities
-
Twenty-seven compounds showed dual anti-cancer and immunomodulatory activities.Series (6a-f) show perceptual inhibition range of 32.1-96.8 for SF-295 cell line.Compounds (6b) and (6f) show better inhibition profile of cancer cell lines than thl.The functionalization of series 3 to series 6 achieved better anti-cancer profile.
- De Oliveira Cardoso, Marcos Veríssimo,Magalh?es Moreira, Diogo Rodrigo,Oliveira Filho, Gevanio Bezerra,Tiburcio Cavalcanti, Suellen Melo,Duarte Coelho, Lucas Cunha,Pontes Espíndola, José Wanderlan,Rubio Gonzalez, Laura,Montenegro Rabello, Marcelo,Zaldini Hernandes, Marcelo,Pinheiro Ferreira, Paulo Michel,Pessoa, Cláudia,De Simone, Carlos Alberto,Teixeira Guimar?es, Elisalva,Pereira Soares, Milena Botelho,Lima Leite, Ana Cristina
-
p. 491 - 503
(2015/05/13)
-
- Discovery of phthalimides as immunomodulatory and antitumor drug prototypes
-
Optimized anticancer agents: A set of functionalized phthalimides was synthesized and evaluated for antitumor activities and as modulators of the secretion of cytokines and nitric oxide. Their potency was compared with that of thalidomide, and as a result, a new potent anticancer and immunomodulatory agent, compound 2b, was identified.
- Pessoa, Claudia,Ferreira, Paulo Michel P.,Lotufo, Leticia Veras C.,DeMoraes, Manoel O.,Cavalcanti, Suellen M. T.,Coelho, Lucas Cunha D.,Hernandes, Marcelo Z.,Leite, Ana Cristina L.,DeSimone, Carlos A.,Costa, Vlaudia M. A.,Souza, Valdenia M. O.
-
scheme or table
p. 523 - 528
(2010/12/25)
-
