RESUMO
Results of studies on the antitumor activity of 26 newly synthetized 1-nitro-9-aminoacridine derivatives by means of in vitro and in vivo tests are presented. 15 derivatives among those showed repeated activity against the sarcoma growth. There were compounds with alkylaminopropyl chains, with hydroxyalkyl-aminoalkyl chains and also with hydroxyalkyl chains on amino group of 1-nitro-9-aminoacridine molecule. The other compounds with aminoacids in position 9 of 1-nitroacridine were active at higher doses. The remaining 7 compounds did not show any antitumor activity. Some aspects of the cellular antineoplastic response, as well as the morphologic appearance of the tumor invasion zone, were studied in comparison with the results of the screening tests. It seems that apart from the structural similarity each derivative has an individual influence on the host reactivity during the tumor growth.
Assuntos
Aminoacridinas/farmacologia , Antineoplásicos/farmacologia , Animais , Humanos , Técnicas In Vitro , Ativação Linfocitária/efeitos dos fármacos , Camundongos , Fagocitose/efeitos dos fármacos , Plantas , Sarcoma 180/tratamento farmacológico , Relação Estrutura-AtividadeRESUMO
Results of the studies on antitumor activity of 20 acridines and related compounds (19 of them were new) in Sa-180-bearing mice are presented. Only several of these compounds i.e. C-258, C-829, C-874, and C-899(21) appeared to inhibit the Sa-180 growth; the activity of the two other compounds (C-783(21) and C-755(21)) requires confirmation in further experiments. The remaining 14 compounds were inactive. Some other general effects exerted by the compounds tested in Sa-180-bearing mice and some aspects of the structure-activity relationship are discussed.
Assuntos
Acridinas/uso terapêutico , Antineoplásicos/uso terapêutico , Carbazóis/uso terapêutico , Nitrocompostos/uso terapêutico , Nitroquinolinas/uso terapêutico , Sarcoma Experimental/tratamento farmacológico , Aminoacridinas/uso terapêutico , Aminoquinolinas/uso terapêutico , Animais , Feminino , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Sarcoma Experimental/patologiaRESUMO
Results of the studies on antitumor activity of 12 new 1-nitro-9-alkylaminoalkylaminacridines in mice bearing Sa-180 are presented. Only one of these compounds, viz. C-846 was active repeatedly in Sa-180 test; the activity of 5 other compounds tested (C-845, C-848, C-852, C-865 and C-866) requires further elucidation by means of new tests with Sa-180. The remaining 6 compounds were inactive. Some other general effects in mice bearing Sa-180 and some aspects of the structure-activity relationship are discussed.
Assuntos
Acridinas/uso terapêutico , Sarcoma 180/tratamento farmacológico , Animais , Avaliação Pré-Clínica de Medicamentos , Feminino , Humanos , Masculino , Camundongos , Transplante de Neoplasias , Nitracrina/análogos & derivados , Nitracrina/uso terapêutico , Relação Estrutura-AtividadeRESUMO
Results of studies on the antitumor activity of six 9-aminoacridine derivatives, four 3-nitro-9-aminoacridine derivatives, four 1-nitro-9-aminoacridine derivatives and five N-oxide of 1-nitro-9-aminoacridine derivatives in mice bearing Sa-180 of compound C-709 requires confirmation by further tests with Sa-180. The remaining 15 compounds were inactive. Some other general effects in the mice and some aspects of the structure-activity relationship are discussed.
