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).
CITATION STYLE
Cuartas, V., Crespo, M. D. P., Priego, E. M., Persoons, L., Daelemans, D., Camarasa, M. J., … Pérez-Pérez, M. J. (2019). Design and synthesis of new 6-nitro and 6-Amino-3,3a,4,5-Tetrahydro-2H-Benzo[g]indazole derivatives: Antiproliferative and antibacterial activity. Molecules, 24(23). https://doi.org/10.3390/molecules24234236
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