TY - JOUR
T1 - Design, synthesis and antiproliferative evaluation of fluorenone analogs with DNA topoisomerase i inhibitory properties
AU - Lee, Chia Chung
AU - Chang, Deh Ming
AU - Huang, Kuo Feng
AU - Chen, Chun Liang
AU - Chen, Tsung Chih
AU - Lo, Yang
AU - Guh, Jih Hwa
AU - Huang, Hsu Shan
PY - 2013/11/15
Y1 - 2013/11/15
N2 - A series of 2,7-diamidofluorenones were designed, synthesized, and screened by SRB assay. Some synthesized compounds exhibited antitumor activities in submicromolar range. Ten compounds (3a, 3b, 3c, 3g, 3j, 3l, 4a, 4h, 4i, and 4j) were also selected by NCI screening system and 3c (GI50 = 1.66 μM) appeared to be the most active agent of this series. Furthermore, 3c attenuated topoisomerase I-mediated DNA relaxation at low micromolar concentrations. These results indicated that fluorenones have potential to be further developed into anticancer drugs.
AB - A series of 2,7-diamidofluorenones were designed, synthesized, and screened by SRB assay. Some synthesized compounds exhibited antitumor activities in submicromolar range. Ten compounds (3a, 3b, 3c, 3g, 3j, 3l, 4a, 4h, 4i, and 4j) were also selected by NCI screening system and 3c (GI50 = 1.66 μM) appeared to be the most active agent of this series. Furthermore, 3c attenuated topoisomerase I-mediated DNA relaxation at low micromolar concentrations. These results indicated that fluorenones have potential to be further developed into anticancer drugs.
KW - Fluorenones
KW - NCI 60-cell panel assay
KW - Tilorone
KW - Topoisomerase I
UR - http://www.scopus.com/inward/record.url?scp=84885858566&partnerID=8YFLogxK
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U2 - 10.1016/j.bmc.2013.09.006
DO - 10.1016/j.bmc.2013.09.006
M3 - Article
C2 - 24094433
AN - SCOPUS:84885858566
SN - 0968-0896
VL - 21
SP - 7125
EP - 7133
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 22
ER -