- Synthesis and evaluation of novel podophyllotoxin analogs
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Because prior studies have shown inconsistency between structure-activity relationships for podophyllotoxin derivatives as topoisomerase II inhibitors and cytotoxic agents, eight novel podophyllotoxin analogs were synthesized to further explore the effects of structural variations on both A and D rings on activity. The new compounds contain a 4,5-dimethoxy substituted A ring and opened D-ring variants and were prepared by appropriate functional and stereochemical operations at the methylenedioxy group, C7, C8, and C8′. Four compounds (15, 18, 21 and 22) demonstrated noticeable inhibitory activity against A549, DU145, KB and KBvin tumor cells, and the most active compound 18 showed IC50 values less than 10 μg/mL.
- Li, Jie,Hua, Hui Ming,Tang, Yan Bo,Zhang, Shipeng,Ohkoshi, Emika,Lee, Kuo-Hsiung,Xiao, Zhi Yan
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scheme or table
p. 4293 - 4295
(2012/07/17)
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- Synthesis and anti-HIV-1 activities of novel podophyllotoxin derivatives
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In order to explore the range of biological activities of the podophyllotoxin compound class, a novel series of derivatives of podophyllotoxin, which were conjugates containing stavudine and different structural podophyllotoxin analogues, were designed, synthesized, and evaluated for their anti-HIV-1 activities in vitro. Among these compounds, 19d and 19c showed the highest anti-HIV-1 activities with EC50 values of 0.17 and 0.29 μM and TI values of 466.9 and 354.5, respectively.
- Chen, Shi-Wu,Wang, Yun-Hua,Jin, Yan,Tian, Xuan,Zheng, Yong-Tang,Luo, Du-Qiang,Tu, Yong-Qiang
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p. 2091 - 2095
(2008/02/02)
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- Antitumor agents. I. DNA topoisomerase II inhibitory activity and the structural relationship of podophyllotoxin derivatives as antitumor agents
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Various podophyllotoxin derivatives from desoxypodophyllotoxin (DPT) were synthesized to examine the structural relationships between the biological significance (cytotoxic effect, effects on DNA topoisomerase II and tubulin polymerization) in vitro and a
- Terada,Fujimoto,Nomura,Yamashita,Kobunai,Takeda,Wierzba,Yamada,Yamaguchi
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p. 2720 - 2727
(2007/10/02)
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- Antitumor agents. 124. New 4β-substituted aniline derivatives of 6,7-O,O- demethylene-4'-O-demethylpodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II
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A series of 6,7-O,O-demethylene-4'-O-demethyl-4β-(substituted anilino)-4- desoxypodophyllotoxins (18-23), 6,7-O,O-demethylene-6,7-O,O-dimethyl-4'-O- demethyl-4β-(substituted anilino)-4-desoxypodophyllotoxins (28-31), and their corresponding 4'-O-methyl an
- Wang,Hu,Chen,Cheng,Lee
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p. 871 - 877
(2007/10/02)
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