New spiroindolinones bearing 5-chlorobenzothiazole moiety
| Autor: | Görkem Ermut, Nurten Ozsoy, Nilgün Karalı, Ayse Can |
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| Rok vydání: | 2013 |
| Předmět: |
Indoles
Free Radicals DPPH Stereochemistry Radical Antineoplastic Agents Antioxidants Lipid peroxidation chemistry.chemical_compound Structure-Activity Relationship Picrates Cell Line Tumor Drug Discovery Moiety Humans Spiro Compounds Benzothiazoles Cell Proliferation Pharmacology Indole test Ethanol ABTS Dose-Response Relationship Drug Molecular Structure Chemistry Biphenyl Compounds General Medicine Benzothiazole Lipid Peroxidation Drug Screening Assays Antitumor Sulfonic Acids |
| Zdroj: | Journal of enzyme inhibition and medicinal chemistry. 29(4) |
| ISSN: | 1475-6374 |
| Popis: | In this study, 5-chloro-3H-spiro-[1,3-benzothiazole-2,3'-indole]-2'(1'H)-one derivatives 3a-l were synthesized by the reaction of 1H-indole-2,3-diones 1a-l with 2-amino-4-chlorothiophenol 2 in ethanol. 3a-l were tested for their abilities to inhibit lipid peroxidation (LP), scavenge DPPH(•) and ABTS(•+) radicals, and to reduce Fe(3+) to Fe(2+). Most of the tested compounds exhibited potent scavenging activities against ABTS(•+) radical, reducing powers and strong inhibitory capacity on LP. 3 a, 3 d, 3 e, 3h, 3 j and 3 k chosen as prototypes were evaluated in the National Cancer Institute's in vitro primary anticancer assay. The greatest growth inhibitions were observed against a non-small cell lung cancer cell line HOP-92 for R1-fluoro substituted 3 d and a renal cancer cell line RXF-393 for R-chloro substituted 3 e in the primary screen. |
| Databáze: | OpenAIRE |
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