Citation: Ji Wu RUAN, Zhi Shu HUANG, Jin Feng HUANG, Cui Juan DU, Shi Liang HUANG, Zhi SHI, Li Wu FU, Lian Quan GU. Synthesis of Phenoxazinone Derivatives and Antiproliferative Activities on Wild-type and Drug-resistant Tumor Cells[J]. Chinese Chemical Letters, ;2006, 17(9): 1141-1144. shu

Synthesis of Phenoxazinone Derivatives and Antiproliferative Activities on Wild-type and Drug-resistant Tumor Cells

1.
School of Pharmaceutical Sciences, Zhongshan University, Guangzhou 510080;
2.
Cancer Center, Sun Yet-sen University, Guangzhou 510060

Received Date: 1 March 2006

Fund Project: The authors gratefully acknowledge the financial support by the National Natural Science Foundation of China (No. 20472117), the Science Foundation of Zhuhai (PC20041131), and the Scientific Research Foundation for the Returned Overseas Chinese Scholars.

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 MTT assay. The results showed that most of them inhibited cell proliferation in a submicromolar to micromolar 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.
- Antitumor,
- phenoxazinones,
- iminoquinones,
- multidrug-resistance
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1.
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