Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties
| Autor: | Zhan-Cheng Li, Yun-Zhou Jin, Nan Ma, Lin Xiao, Quan-Hai Liu, Rong-Hua Zhang, Da-Xu Fu |
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| Jazyk: | angličtina |
| Rok vydání: | 2011 |
| Předmět: |
Indoles
synthesis Stereochemistry Substituent Pharmaceutical Science Antineoplastic Agents Indolin 2 one antitumor activities indolin-2-one chloropyrrole Ring (chemistry) Article Analytical Chemistry lcsh:QD241-441 chemistry.chemical_compound Mice lcsh:Organic chemistry Cell Line Tumor Drug Discovery medicine Molecule Animals Humans Pyrroles Physical and Theoretical Chemistry Pyrrole Cardiotoxicity Molecular Structure Chemistry Melanoma Organic Chemistry medicine.disease Vascular Endothelial Growth Factor Receptor-2 respiratory tract diseases Chemistry (miscellaneous) Cell culture Molecular Medicine Intercellular Signaling Peptides and Proteins Chlorine Drug Screening Assays Antitumor |
| Zdroj: | Molecules, Vol 16, Iss 11, Pp 9368-9385 (2011) Molecules; Volume 16; Issue 11; Pages: 9368-9385 Molecules |
| ISSN: | 1420-3049 |
| Popis: | Eighteen novel 3-substituted-indolin-2-ones containing chloropyrroles were synthesized and their biological activities were evaluated. The presence of a chlorine atom on the pyrrole ring was crucial to reduce cardiotoxicity. The presence of a 2-(ethyl-amino)ethylcarbamoyl group as a substituent at the C-4' position of the pyrrole enhanced the antitumor activities notably. IC50 values as low as 0.32, 0.67, 1.19 and 1.22 μM were achieved against non-small cell lung cancer (A549), oral epithelial (KB), melanoma (K111) and large cell lung cancer cell lines (NCI-H460), respectively. |
| Databáze: | OpenAIRE |
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