A series of novel phenoxazinone derivatives (1-6) were designed and synthesized for evaluating their antitumor activities. The antiproliferative activities of the prepared compounds against representative human neop...A series of novel phenoxazinone derivatives (1-6) were designed and synthesized for evaluating their antitumor activities. The antiproliferative activities of the prepared compounds against representative human neoplastic cell lines were evaluated by MTF assay. The results showed that most of them inhibited cell proliferation in a submicromolar to rnicromolar range. These compounds were also evaluated against KBv200 and MCF-7/Adr cell lines, which overexpress the MDR/P-glycoprotein drug efflux pump responsible for drug resistance, and had a more potential for resisting MDR than their lead compound APO.展开更多
A series of novel coumarin-stilbenes hybrids called 3-arylcoumarins were synthesized via Perkin reaction and evaluated as potential antitumor agents.The results showed that some compounds exhibited in vitro activity a...A series of novel coumarin-stilbenes hybrids called 3-arylcoumarins were synthesized via Perkin reaction and evaluated as potential antitumor agents.The results showed that some compounds exhibited in vitro activity against KB,KV,MCF-7,MCF-7/ ADR cell lines to some extent.Compound 3a showed remarkable effect against KB tumor cells with an IC50 value of 5.18μmol/L.展开更多
基金support by the National Natural Science Foundation of China(No.20472117)the Science Foundation of Zhuhai(PC20041131)the Scientific Research Foundation for the Returned 0verseas Chinese Scholars.
文摘A series of novel phenoxazinone derivatives (1-6) were designed and synthesized for evaluating their antitumor activities. The antiproliferative activities of the prepared compounds against representative human neoplastic cell lines were evaluated by MTF assay. The results showed that most of them inhibited cell proliferation in a submicromolar to rnicromolar range. These compounds were also evaluated against KBv200 and MCF-7/Adr cell lines, which overexpress the MDR/P-glycoprotein drug efflux pump responsible for drug resistance, and had a more potential for resisting MDR than their lead compound APO.
基金National Key Technology R&D Program,Science and Technology Program of Guangdong Province and Strategic Cooperation Program between Guangdong Province and Chinese Academy of Sciences,PR China(Nos. 2007BAD82B02,2006B35604002,and 2009B091300125) for financial support
文摘A series of novel coumarin-stilbenes hybrids called 3-arylcoumarins were synthesized via Perkin reaction and evaluated as potential antitumor agents.The results showed that some compounds exhibited in vitro activity against KB,KV,MCF-7,MCF-7/ ADR cell lines to some extent.Compound 3a showed remarkable effect against KB tumor cells with an IC50 value of 5.18μmol/L.