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Chrysin-benzothiazole conjugates as antioxidant and anticancer agents
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SYSNO ASEP 0451908 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Chrysin-benzothiazole conjugates as antioxidant and anticancer agents Tvůrce(i) Mistry, B.M. (KR)
Patel, Rahul V. (UEB-Q)
Keum, Y.S. (KR)
Kim, D.H. (KR)Zdroj.dok. Bioorganic and Medicinal Chemistry Letters. - : Elsevier - ISSN 0960-894X
Roč. 25, č. 23 (2015), s. 5561-5565Poč.str. 5 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova Chrysin ; Benzothiazole ; Cervical cancer Vědní obor RIV EB - Genetika a molekulární biologie CEP LO1204 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Institucionální podpora UEB-Q - RVO:61389030 UT WOS 000364535400021 DOI 10.1016/j.bmcl.2015.10.052 Anotace 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. Pracoviště Ústav experimentální botaniky Kontakt David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Rok sběru 2016
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