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Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of 2-phenyl- or hydroxylated 2-phenyl-4-aryl-5H-indeno[1,2-b]pyridines
- Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of 2-phenyl- or hydroxylated 2-phenyl-4-aryl-5H-indeno[1,2-b]pyridines
- Kadayat T.M.; Song C.; Shin S.; Magar T.B.T.; Bist G.; Shrestha A.; Thapa P.; Na Y.; Kwon Y.; Lee E.-S.
- Ewha Authors
- SCOPUS Author ID
- Issue Date
- Journal Title
- Bioorganic and Medicinal Chemistry
- vol. 23, no. 13, pp. 3499 - 3512
- Anticancer agents; Cytotoxicity; Hydroxylated 2-phenyl-4-aryl-5Hindeno[1,2-b]pyridines; Topoisomerase I and II inhibitor
- Elsevier Ltd
- SCI; SCIE; SCOPUS
- Abstract A series of novel twenty-eight rigid 2-phenyl- or hydroxylated 2-phenyl-4-aryl-5H-indeno[1,2-b]pyridines were synthesized and evaluated for their topoisomerase inhibitory activity as well as their cytotoxicity against several human cancer cell lines. Generally, hydroxylated compounds (16-18, 22-25, and 29-31) containing furyl or thienyl moiety at 4-position of central pyridine exhibited strong topoisomerase I and II inhibitory activity compared to positive control, camptothecin and etoposide, respectively, in low micromolar range. Structure-activity relationship study revealed that indenopyridine compounds with hydroxyl group at 2-phenyl ring in combination with furyl or thienyl moiety at 4-position are important for topoisomerase inhibition. Compounds (22-25) which contain hydroxyl group at meta position of the 2-phenyl ring at 2-position and furanyl or thienyl substitution at 4-position of indenopyridine, showed concrete correlations between topo I and II inhibitory activity, and cytotoxicity against evaluated human cancer cell lines. © 2015 Elsevier Ltd.
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