1376687-00-1Relevant articles and documents
Benzo[a]phenazine derivatives: Promising scaffolds to combat resistant Mycobacterium tuberculosis
Halicki, Priscila Cristina Bartolomeu,da Silva, Eufranio Nunes,Jardim, Guilherme Augusto de Melo,Almeida, Renata Gomes de,Vicenti, Juliano Rosa de Menezes,Gon?alves, Bruna Lisboa,da Silva, Pedro Eduardo Almeida,Ramos, Daniela Fernandes
, p. 352 - 362 (2021/06/30)
The continuous emergence of resistant Mycobacterium tuberculosis keeps tuberculosis (TB) treatment options still insufficient, and new therapeutic alternatives are urgently needed. Considering the antimycobacterial activity of phenazine derivatives previously reported by our research group, we aimed to explore possible applications to circumvent the resistance in M. tuberculosis. Firstly, we evaluated the antimicrobial activity of seven benzo[a]phenazine derivatives against eleven M. tuberculosis strains: ten resistant and one susceptible (H37Rv). Then, we determined the cytotoxicity of benzo[a]phenazine derivatives and investigated the possible mechanism of action of the most promising compound. Among them, compound 10 was the only one active against all strains evaluated, with a minimum inhibitory concentration between 18.3 and 146.5?μM. For some resistant strains, this compound showed antimicrobial activity higher than rifampicin and it was also active against MDR strains, indicating an absence of cross-resistance with anti-TB drugs. Also, 10 showed a pharmacological safety for further in vivo studies and its mechanism of action seems to be related to oxidative stress. Thus, our findings indicate that benzo[a]phenazine derivatives are promising scaffolds for the development of new anti-TB drugs, mainly focusing on the treatment of resistant TB cases.
Synthesis and evaluation of the cytotoxic activity of 1,2- furanonaphthoquinones tethered to 1,2,3-1H-triazoles in myeloid and lymphoid leukemia cell lines
Cardoso, Mariana F.C.,Rodrigues, Patrícia C.,Oliveira, Maria Eduarda I.M.,Gama, Ivson L.,Da Silva, Illana M.C.B.,Santos, Isabela O.,Rocha, David R.,Pinho, Rosa T.,Ferreira, Vitor F.,De Souza, Maria Cecília B.V.,Da Silva, Fernando De C.,Silva-Jr, Floriano Paes
, p. 708 - 717 (2014/08/18)
Leukemia is the most common blood cancer, and its development starts at diverse points, leading to distinct subtypes that respond differently to therapy. This heterogeneity is rarely taken into account in therapies, so it is still essential to look for ne
Potent naphthoquinones against antimony-sensitive and -resistant Leishmania parasites: Synthesis of novel α- And nor-α-lapachone-based 1,2,3-triazoles by copper-catalyzed azide-alkyne cycloaddition
Guimar?es, Tiago T.,Pinto, Maria Do Carmo F.R.,Lanza, Juliane S.,Melo, Maria N.,Do Monte-Neto, Rubens L.,De Melo, Isadora M.M.,Diogo, Emilay B.T.,Ferreira, Vitor F.,Camara, Celso A.,Valen?a, Wagner O.,De Oliveira, Ronaldo N.,Frézard, Frédéric,Da Silva Júnior, Eufranio N.
, p. 523 - 530 (2013/07/27)
Continuing our screening program for novel anti-parasite compounds, we synthesized seven 1,4-naphthoquinones coupled to 1,2,3-triazoles, five nor-β-lapachone-based 1,2,3-triazoles and ten α-lapachone-based 1,2,3-triazoles. These and other naphthoquinonoid