期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 15, 页码 5502-5510出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm1001698
关键词
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资金
- National Nature Science Foundation of China [30971137, 20832007, 20802087]
- National Basic Research Program of China (973 Program) [2010CB833300]
- Ministry of Health [2009ZX09501-007, 2009ZX09501-016]
Compound 1 ((-)-gossypol) has been long known as a chemical anticancer agent. With its low water solubility and toxicity, it is not widely used as a commercial drug. To overcome these disadvantages, several novel derivatives of gossypol were designed, synthesized, and analyzed. One of the derivatives, compound 7 (6-aminopenicillanic acid sodium-gossypolone), was identified with great water solubility and anticancer property, suggested by inducing a dramatically decrease in Bcl-2 and Bcl-xL protein expression level found in vitro and growth inhibition of murine colon tumor in vivo. Furthermore, it was also recognized with less toxicity than compound 1 in vivo and significantly increased chemotherapeutic sensitivity against colon cancer in combination with traditional chemotherapeutic agent 5-fluorouracil. Therefore, it is concluded that compound 7 is superior to parent compound 1, and further preclinical studies of compound 7 is necessary for colon cancer therapy.
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