Synthesis of a rhodanine-based compound library targeting Bcl-XL and Mcl-1

Paul H. Bernardo, Thirunavukkarasu Sivaraman, Kah-Fei Wan, Jin Xu, Janarthanan Krishnamoorthy, Chun Meng Song, Liming Tian, Jasmine S. F. Chin, Diane S. W. Lim, Henry Y. K. Mok, Victor C. Yu, Joo Chuan Tong (+1 others)
2011 Pure and Applied Chemistry  
A small library of pyridine-based rhodanine analogues of BH3I-1 were synthesized and screened against B-cell lymphoma-extra large (Bcl-XL) and myeloid cell leukemia sequence 1 (Mcl-1) for the ability to displace 5-carboxyfluorescein-labeled Bak peptide (Flu-Bak). Differences in selectivity toward Bcl-XL and Mcl-1 were observed, and the binding modes of selected compounds were studied further. The results may be useful in designing potent small-molecule inhibitors of Bcl-XL and Mcl-1 as well as selective Mcl-1 inhibitors.
doi:10.1351/pac-con-10-10-29 fatcat:eallo6nqnzfzzhfrww2imniv4e