<P>A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HC...
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https://www.riss.kr/link?id=A107741365
Thapa, P. ; Kadayat, T.M. ; Park, S. ; Shin, S. ; Thapa Magar, T.B. ; Bist, G. ; Shrestha, A. ; Na, Y. ; Kwon, Y. ; Lee, E.S.
2016
-
SCOPUS,SCIE
학술저널
145-159(15쪽)
0
상세조회0
다운로드다국어 초록 (Multilingual Abstract)
<P>A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HC...
<P>A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HCT15, T47D, DU145, and Hela. Most of the tested compounds exhibited stronger topo II inhibitory activity at 100 mu M as compared to etoposide. All the compounds, except 39, did not show topo I inhibitory activity. Interestingly, compounds that showed better topo II inhibition than etoposide have ortho-or para-chlorophenyl at 4-position of central pyridine, and none of the compounds possess meta-chlorophenyl. SAR study revealed the importance of ortho-or para-chlorophenyl at 4-position of the central pyridine for selective topo II inhibitory activity. Similarly, all compounds possessing meta-or para-hydroxyphenyl moieties showed moderate to significant cytotoxic effects. Particularly, compounds 27-37, and 39 which showed excellent cytotoxicity (IC50 = 0.68-1.25 mu M) against T47D breast cancer cells suggest the importance of meta-or para-hydroxyphenyl moiety at 2-position of the central pyridine for the design of anticancer agents with related scaffolds. (C) 2016 Elsevier Inc. All rights reserved.</P>
Bioactivity-guided isolation of antioxidant triterpenoids from Betula platyphylla var. japonica bark