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1.
Biochem Pharmacol ; 199: 114991, 2022 05.
Artigo em Inglês | MEDLINE | ID: mdl-35288151

RESUMO

Carbon monoxide has recently emerged to promote tissue regeneration, enhance the innate immune system, and have anti-inflammatory and antibacterial properties. While the first generation Ru(II) carbonyl prodrugs (CORM-2 and CORM-3) displayed several beneficial biological effects, a search in the literature shows that little work has been done to address the drawbacks of CORM-2/-3, exploring other CO triggered methods for the next generation Ru(CO)2II based compounds and examining their valuable biological impact. We present a summary of most work related to Ru(II) carbon monoxide-releasing molecules, protein bioconjugation, and antibacterial and anti-inflammatory properties.


Assuntos
Compostos Organometálicos , Rutênio , Antibacterianos/química , Anti-Inflamatórios/farmacologia , Monóxido de Carbono/metabolismo , Monóxido de Carbono/farmacologia , Compostos Organometálicos/farmacologia , Rutênio/química , Rutênio/farmacologia
2.
Eur J Med Chem ; 53: 403-7, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22583778

RESUMO

The present work reports the synthesis of some new Schiff bases, 5-(substituted benzylideneamino)-6-cyano-7H-7-(4-methoxyphenyl)-2-(4-sulphamoylphenylamino) pyrano[2,3-d]thiazole (5-15). The design of the structures of these compounds complies with the general pharmacophoric requirements for CA inhibiting anticancer drugs. The newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Most of the screened compounds showed interesting cytotoxic activities compared to doxorubicin as a reference drug. Compounds 4, 6-8 and 11 (IC(50): 27.51, 10.25, 9.55, 9.39 and 9.70 µM, respectively) exhibited higher cytotoxic activities than the reference drug doxorubicin (IC(50): 32.00 µM). Additionally, the previously mentioned compounds were evaluated again for their ability to enhance the cell killing effect of γ-radiation.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Radiossensibilizantes/química , Radiossensibilizantes/farmacologia , Sulfonamidas/química , Tiazóis/química , Tiazóis/farmacologia , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos da radiação , Desenho de Fármacos , Raios gama , Humanos , Concentração Inibidora 50 , Radiossensibilizantes/síntese química , Bases de Schiff/química , Tiazóis/síntese química
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