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Chrysin-benzothiazole conjugates as antioxidant and anticancer agents
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SYSNO ASEP 0451908 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Chrysin-benzothiazole conjugates as antioxidant and anticancer agents Author(s) Mistry, B.M. (KR)
Patel, Rahul V. (UEB-Q)
Keum, Y.S. (KR)
Kim, D.H. (KR)Source Title Bioorganic and Medicinal Chemistry Letters. - : Elsevier - ISSN 0960-894X
Roč. 25, č. 23 (2015), s. 5561-5565Number of pages 5 s. Language eng - English Country GB - United Kingdom Keywords Chrysin ; Benzothiazole ; Cervical cancer Subject RIV EB - Genetics ; Molecular Biology R&D Projects LO1204 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Institutional support UEB-Q - RVO:61389030 UT WOS 000364535400021 DOI https://doi.org/10.1016/j.bmcl.2015.10.052 Annotation 7-(4-Bromobutoxy)-5-hydroxy-2-phenyl-4H-chromen-4-one, obtained from chrysin with 1,4-dibromobutane, was combined with a wide range of 6-substituted 2-aminobenzthiazoles, which had been prepared from the corresponding anilines with potassium thiocyanate. Free radical scavenging efficacies of newer analogues were measured using DPPH and ABTS assays, in addition to the assessment of their anticancer activity against cervical cancer cell lines (HeLa and CaSki) and ovarian cancer cell line (SK-OV-3) implementing the SRB assay. Cytotoxicity of titled compounds was checked using Madin-Darby canine kidney (MDCK) non-cancer cell line. Overall, 6a-r indicated remarkable antioxidant power as DPPH center dot and ABTS(center dot+) scavengers; particularly the presence of halogen(s) (6g, 6h, 6j-6l) was favourable with IC50 values comparable to the control ascorbic acid. Unsubstituted benzothiazole ring favored the activity of resultant compounds (6a and 6r) against HeLa cell line, whereas presence of chlorine (6g) or a di-fluoro group (6k) was a key to exert strong action against CaSki. Moreover, a mono-fluoro (6j) and a ketonic functionality (6o) were beneficial to display anticipated anticancer effects against ovarian cancer cell line SK-OV-3. The structural assignments of the new products were done on the basis of IR, H-1 NMR, C-13 NMR spectroscopy and elemental analysis. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2016
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