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

被引：5

作者：

Cuartas, Viviana ^{[1
,2
]}

Crespo, Maria del Pilar ^{[3
]}

Priego, Eva-Maria ^{[4
]}

Persoons, Leentje ^{[5
]}

Daelemans, Dirk ^{[5
]}

Camarasa, Maria-Jose ^{[4
]}

Insuasty, Braulio ^{[1
,2
]}

Perez-Perez, Maria-Jesus ^{[4
]}

机构：

[1] Univ Valle, Dept Quim, Grp Invest Compuestos Heterocicl, Cali 25360, Colombia

[2] Ctr Bioinformat & Photon CIBioFI, Calle 13 100-00,Edificio E20,1069, Cali 760032, Colombia

[3] Univ Valle, Dept Microbiol, Grp Biotecnol & Infecc Bacterianas, Cali 760043, Colombia

[4] CSIC, Inst Quim Med, Juan Cierva 3, E-28006 Madrid, Spain

[5] Katholieke Univ Leuven, Rega Inst Med Res, Lab Virol & Chemotherapy, Dept Microbiol Immunol & Transplantat, Herestr 49, B-3000 Leuven, Belgium

来源：

MOLECULES | 2019年 / 24卷 / 23期

关键词：

indazole; 2-benzylidene-1-tetralone; antiproliferative activity; antibacterial activity; IN-VITRO; NECROPTOSIS INHIBITORS; BIOLOGICAL EVALUATION; PYRAZOLE; RECEPTOR; LIGANDS; TUBULIN; AGENTS;

D O I：

10.3390/molecules24234236

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu M 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 mu g/mL against N. gonorrhoeae with no hemolytic activity in human red blood cells (RBC).

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页数：18

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