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1.
Drug Res (Stuttg) ; 65(1): 9-17, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25116256

RESUMO

A new series of novel substituted 3,4-dihydronaphthalene incorporated to benzo[h]quinoline, benzo[g]indazole, thiazolidin-4-one, pyrazolo[3,4-d]thiazol and thiazolo[4,5-b]pyridine ring systems were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. Some of the tested compounds exhibited promising carcinoma growth inhibition. The detailed synthesis, spectroscopic data and biological activities of the tested compounds were reported.


Assuntos
Antineoplásicos/farmacologia , Naftalenos/farmacologia , Neoplasias/tratamento farmacológico , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Humanos , Naftalenos/síntese química , Naftalenos/química , Neoplasias/patologia , Análise Espectral
2.
Arch Pharm Res ; 26(5): 358-66, 2003 May.
Artigo em Inglês | MEDLINE | ID: mdl-12785731

RESUMO

Some N-p-substituted phenyl uracil-5-sulphonamide derivatives have been synthesized to be evaluated as molluscicides against Biomphalanaria alexandrina snails, the intermediate host of Schistosoma mansoni. Schistosoma mansoni infected mice were treated with hemolymph obtained from pre-treated Biomphalana alexandrina snails with the products 4a, 10a, 10b and 4b or obtained from non-treated snails. The selection of the concentration based on the predetermined dose which caused mortality of less than 50% of snails/24 h. LC50 of compounds 4a, 10a, 10b and 4b was 50, 100, 200 and 50 ppm respectively. The result showed that immunostimulatory effect of treated hemolymph with compounds 4a, 10a and 4b was related to significant protective effects (44.4, 34.6 and 50.4% reduction in worm burden respectively). In addition, mean total worm burdens were significantly reduced in non treated hemolymph by 33.8%. The effect of hemolymph obtained from treated or non treated snails on S. mansoni adult worms antigens was studied by indirect immunofluorescence technique using chronic mouse sera (CMS). The results indicated that there was a strong reaction with epitopes in gut epithelium, tubercles, teigument and subtegumental musculature of untreated and treated S. mansoni adult worms antigens. Therefore, treatment of hemolymph obtained from pre-treated snails with compounds 4a, 10a, and 4b can stimulate specific immune response and induce protective effects against S. mansoni infection.


Assuntos
Adjuvantes Imunológicos/síntese química , Biomphalaria/efeitos dos fármacos , Hemolinfa/efeitos dos fármacos , Esquistossomose mansoni/prevenção & controle , Sulfonamidas/síntese química , Uracila/análogos & derivados , Uracila/síntese química , Adjuvantes Imunológicos/farmacologia , Animais , Antígenos de Helmintos/imunologia , Antiparasitários/síntese química , Antiparasitários/farmacologia , Biomphalaria/imunologia , Biomphalaria/parasitologia , Morte , Feminino , Hemolinfa/imunologia , Interações Hospedeiro-Parasita , Masculino , Camundongos , Moluscocidas/síntese química , Moluscocidas/farmacologia , Schistosoma mansoni/fisiologia , Esquistossomose mansoni/imunologia , Esquistossomose mansoni/parasitologia , Razão de Masculinidade , Sulfonamidas/farmacologia , Uracila/farmacologia
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