Design,synthesis and antiproliferative evaluation of fluorenone analogs with DNA topoisomerase I inhibitory properties |
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| Authors: | Chia-Chung Lee Deh-Ming Chang Kuo-Feng Huang Chun-Liang Chen Tsung-Chih Chen Yang Lo Jih-Hwa Guh Hsu-Shan Huang |
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| Institution: | 1. Graduate Institute of Life Sciences, National Defense Medical Center, Taipei 114, Taiwan;2. School of Pharmacy, National Defense Medical Center, Taipei 114, Taiwan;3. Rheumatology/Immunology/Allergy, Tri-Service General Hospital, National Defense Medical Center, Taipei 114, Taiwan;4. Department of Oncology and of Obstetrics and Gynecology, Chi-Mei Foundation Medical Center, Tainan 710, Taiwan;5. School of Pharmacy, National Taiwan University, Taipei 100, Taiwan;6. School of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan |
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| Abstract: | 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. |
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| Keywords: | Tilorone Fluorenones Topoisomerase I NCI 60-cell panel assay |
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