J4 ›› 2010, Vol. 45 ›› Issue (5): 1-5.

• Articles •     Next Articles

The instance of new drug research and development: novel anti-cancer lead compounds of 4-thiazolidinones

LIU Xiao-jun1, YAN Bing2*   

  1. 1.School of Pharmaceutical Science, Shandong University, Jinan 250012, Shandong, China;
    2. School of Chemistry and Chemical Engineering,  Shandong University, Jinan 250100, Shandong, China
  • Received:2010-03-02 Online:2010-05-16 Published:2010-05-24


Taking thiazolidinone compounds as an example, we discuss the processes leading to the discovery of anti-cancer lead compounds. Using combinatorial chemistry and high throughput screening approaches, we discovered potent compounds against drugresistant cancer cells. Mechanistic studies indicated that these compounds inhibited microtubule formation, caused G2/M arrest in cell cycle, and induced apoptosis and autophagy. The anticancer activity did not depend on the status of P-gp in cells. These compounds had superb membrane permeability and inhibited tumor growth in vivo. Screening them against 60 human cancer cell lines demonstrated broad anti-cancer activities indicating that they will play a significant role in the future of our fight against cancer.

Key words: combinatorial chemistry; thiazolidinone; selectivity; anti-cancer

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