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

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

机构信息

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.

出版信息

Molecules. 2019 Nov 21;24(23):4236. doi: 10.3390/molecules24234236.

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 , , 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).

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4777/6930490/917b9069cf97/molecules-24-04236-g001.jpg

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