| Autor: |
El Ashry el SH; International Center for Chemical and Biological Sciences, H.E.J. Research Institute of Chemistry, Karachi University, Karachi, Pakistan. eelashry60@hotmail.com, El Tamany el SH, Abd El Fattah Mel D, Aly MR, Boraei AT, Mesaik MA, Abdalla OM, Fatima B, Jabeen A, Shukrulla A, Soomro S |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2013 Feb; Vol. 28 (1), pp. 105-12. Date of Electronic Publication: 2011 Dec 06. |
| DOI: |
10.3109/14756366.2011.636361 |
| Abstrakt: |
A series of S- and N-alkylated indolyloxadiazoles 2-7 were prepared. All compounds were tested for their immunomodulatory activity against T-cell proliferation, oxidative burst and cytokine analysis. Compounds 1, 2a, 2b, 2c and 2k demonstrated highly significant (P ≤ 0.005) inhibition on PHA activated T-cell proliferation with IC(50) less than 3 µg/mL concentration, while 3b exert a moderate inhibitory effect with IC(50) 8.6 µg/mL. Among all compounds of the series, only 2h was found to suppress phagocytes ROS production (IC(50) 2.4 µg/mL) in luminol-based chemiluminescence (CL) assay. Compounds 2a-k have stimulatory effect on proinflammatory cytokine predominantly IL-1β but no effect on IL-4 and NO production indicating that these compounds might have selective inhibitory effect on T-cell proliferation. Cytotoxic effect on T-cell proliferation was tested on NIH-3T3 mouse fibroblast normal cell line. All compounds were found to be free from toxic effects up to 100 μM concentration. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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