Synthesis and evaluation of novel sulfonamide analogues of 6/7-aminoflavones as anticancer agents via topoisomerase II inhibition

[Display omitted] A series of new sulfonamide analogues of 6/7-aminoflavones were synthesized by using molecular hybridization approach. These new sulfonamide analogues were screened for antiproliferative activity against human hepatocellular carcinoma (HepG-2), human lung cancer cell line (A-549),...

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Published in:Bioorganic & medicinal chemistry letters 2020-07, Vol.30 (14), p.127246, Article 127246
Main Authors: Shelke, Rohini N., Pansare, Dattatraya N., Sarkate, Aniket P., Narula, Ishudeep K., Lokwani, Deepak K., Tiwari, Shailee V., Azad, Rajaram, Thopate, Shankar R.
Format: Article
Language:English
Subjects:
Aminoflavones
Anticancer activity
Docking
Sulfonamide
topoisomerase-II
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Summary:[Display omitted] A series of new sulfonamide analogues of 6/7-aminoflavones were synthesized by using molecular hybridization approach. These new sulfonamide analogues were screened for antiproliferative activity against human hepatocellular carcinoma (HepG-2), human lung cancer cell line (A-549), human colorectal adenocarcinoma (Caco-2) cancer cell lines. Compounds 5p, 5q, 5t, 5v, 5w and 5x exhibited good anticancer activity against selected cancer cell lines. These compounds were further evaluated to predict their ability to inhibit topoisomerase-II enzyme. Compound 5x has shown potent antiproliferative activity (IC50 value 0.98 µM) as compared to standard drug Adriamycin (IC50 = 0.94 µM) indicating that these compounds exhibits anticancer activity via inhibition of topoisomerase-II enzyme. Docking results also have supported above observations by indicating that compounds are held in the active pocket by combination of various hydrogen and hydrophobic interactions with Top II-DNA-etoposide enzyme.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2020.127246