Publications (2)5.3 Total impact
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Article: Synthesis and evaluation of novel podophyllotoxin analogs.
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ABSTRACT: 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 IC(50) values less than 10 μg/mL.Bioorganic & medicinal chemistry letters 05/2012; 22(13):4293-5. · 2.65 Impact Factor -
Article: Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors.
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ABSTRACT: Fourteen naphthoquinone derivatives (1-14) were designed based on a putative proteasome inhibitor PI-083. These compounds were synthesized and evaluated against A549, DU145, KB, and KBvin tumor cell lines. Six compounds (2, 4, 8, 9, 10, and 13) showed antiproliferative activities comparable to that of PI-083. Among them, compound 8 was confirmed as a 20S proteasome inhibitor in both in vitro and cell-based assays. These findings endorse further optimization efforts based on this structural phenotype to develop potential anticancer drug candidates.Bioorganic & medicinal chemistry letters 03/2012; 22(8):2772-4. · 2.65 Impact Factor
