In-vitro cytotoxicity of synthesized phthalide-fused indoles and indolines against HL-60 and HepG2 cells
| Autor: | Masayuki Ninomiya, Siti Aishah Hasbullah, Mamoru Koketsu, Wong Sheryn |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Indole test
Chemistry Stereochemistry General Chemical Engineering 02 engineering and technology General Chemistry Conjugated system 010402 general chemistry 021001 nanoscience & nanotechnology 01 natural sciences In vitro 0104 chemical sciences Phthalide lcsh:Chemistry chemistry.chemical_compound lcsh:QD1-999 Cell culture Indoline Potency Moiety 0210 nano-technology |
| Zdroj: | Arabian Journal of Chemistry, Vol 13, Iss 2, Pp 3856-3865 (2020) |
| ISSN: | 1878-5352 |
| DOI: | 10.1016/j.arabjc.2019.02.002 |
| Popis: | Phthalide derivatives bearing indole or indoline moieties were successfully synthesized via eco-friendly method and were evaluated for their antiproliferative activity on HL-60 and HepG2 cell lines in vitro. At a final concentration of 100 μM, most of the compounds showed moderate potency on both the cell lines tested. Compound 3b bearing 5-chloro substituted indoline had the best potency against HL-60 and HepG2 cell lines with IC50 values of 45.4 and 57.7 μM, respectively. It was also found that replacement of a conjugated indoline to indole moiety gave better antiproliferative activity on HL-60 cells by almost two-fold. Morphological observation demonstrated numerous fragmented nuclei which are indicative of apoptosis. Molecular docking studies predicted non-covalent interactions and H-bonding of selected compounds with the P2 binding hot spot of the anti-apoptotic protein, Bcl-2, formed by Asp108, Phe109, Met112, Leu134, Arg143, Ala146 and Val153. Overall, our work highlights the potential of synthesized phthalide-fused indoles or indolines as antitumor agents. Keywords: Phthalide, Indole, Indoline, Antiproliferative activity, Molecular docking |
| Databáze: | OpenAIRE |
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