J4 ›› 2010, Vol. 45 ›› Issue (5): 1-5.
• Articles •
LIU Xiao-jun1, YAN Bing2*
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 drugresistant cancer cells. Mechanistic studies indicated that these compounds inhibited microtubule formation, caused G2／M arrest in cell cycle, and induced apoptosis and autophagy. The anticancer 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.
combinatorial chemistry; thiazolidinone; selectivity; anti-cancer
LIU Xiao-jun1, YAN Bing2*. The instance of new drug research and development: novel anti-cancer lead compounds of 4-thiazolidinones[J].J4, 2010, 45(5): 1-5.
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