Grupo de Investigación de Compuestos Heterocíclicos, Departamento de Química, Universidad del Valle, A. A., Cali 25360, Colombia.
Centre for Bioinformatics and Photonics-CIBioFI, Calle 13 No. 100-00, Edificio E20, No. 1069, Cali 760032, Colombia.
Molecules. 2019 Nov 21;24(23):4236. doi: 10.3390/molecules24234236.
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 , , and have shown IC values between 5-15 μM against the lung carcinoma cell line NCI-H460. Moreover, the nitro compounds were tested for antibacterial activity where compounds and have shown MIC values of 250 and 62.5 μg/mL against with no hemolytic activity in human red blood cells (RBC).
新的取代苯并[g]吲唑通过苯亚甲基四氢萘酮与乙酸中的肼反应合成，带有 6-硝基和 6-氨基基团。对所得的构象约束化合物进行了评估，以研究它们对选定癌细胞系的抗增殖活性。基于硝基的吲唑 、 、 和 对肺癌细胞系 NCI-H460 的 IC 值在 5-15 μM 之间。此外，还对硝基化合物进行了抗菌活性测试，其中化合物 和 对 具有 250 和 62.5 μg/mL 的 MIC 值，对人红细胞（RBC）没有溶血活性。
