Design and Synthesis of New 6-Nitro and 6-Amino-3,3a,4,5-Tetrahydro-2 H-Benzo[ g]indazole Derivatives: Antiproliferative and Antibacterial Activity

新型 6-硝基和 6-氨基-3,3a,4,5-四氢-2 H-苯并[g]吲唑衍生物的设计和合成:抗增殖和抗菌活性

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作者:Viviana Cuartas, María Del Pilar Crespo, Eva-María Priego, Leentje Persoons, Dirk Daelemans, María-José Camarasa, Braulio Insuasty, María-Jesús Pérez-Pérez

Abstract

New substituted benzo[g]indazoles functionalized with a 6-nitro and 6-amino groups have been synthesized by the reaction of benzylidene tetralones with hydrazine in acetic acid. The resulting conformationally-constrained compounds were evaluated for their antiproliferative activity against selected cancer cell lines. The nitro-based indazoles 11a, 11b, 12a and 12b have shown IC50 values between 5-15 μM against the lung carcinoma cell line NCI-H460. Moreover, the nitro compounds were tested for antibacterial activity where compounds 12a and 13b have shown MIC values of 250 and 62.5 μg/mL against N. gonorrhoeae with no hemolytic activity in human red blood cells (RBC).

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