925702-74-5Relevant academic research and scientific papers
Identification of 3,5,6-substituted indolin-2-one's inhibitors of Aurora B by development of a luminescent kinase assay
Zhang, Leilei,Yang, Tianming,Xie, Xilei,Liu, Gang
, p. 2937 - 2942 (2015)
Aurora B kinase plays an important role in the cell normal mitosis and overexpresses in a variety of tumors. Inhibition of Aurora B kinase resulted in an apoptosis of cancer cells, which prevented tumor growth in xenograft models. In this Letter, we developed a luminescent kinase assay to perform high-throughput screening for identification of small molecule Aurora B inhibitors. Two 3,5,6-substituted indolin-2-one derivatives were identified within an in-house compound library. Their new derivatives were then designed and synthesized that resulting two new inhibitors of Aurora B kinase with improved potency. Docking simulation further demonstrated the proposed binding modes between indolin-2-one inhibitor and Aurora B.
Benzimidazole-based compounds kill Mycobacterium tuberculosis
Gong, Yaling,Somersan Karakaya, Selin,Guo, Xiaoyong,Zheng, Purong,Gold, Ben,Ma, Yao,Little, David,Roberts, Julia,Warrier, Thulasi,Jiang, Xiuju,Pingle, Maneesh,Nathan, Carl F.,Liu, Gang
, p. 336 - 353 (2014/03/21)
Tuberculosis remains one of the deadliest infectious diseases, killing 1.4 million people annually and showing a rapid increase in cases resistant to multiple drugs. New antibiotics against tuberculosis are urgently needed. Here we describe the design, sy
