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Title: Synthesis of a rhodanine-based compound library targeting Bcl-XL and Mcl-1
Authors: Bernardo, P.H.
Sivaraman, T.
Wan, K.-F.
Xu, J.
Krishnamoorthy, J.
Song, C.M.
Tian, L.
Chin, J.S.F.
Lim, D.S.W.
Mok, H.Y.K. 
Yu, V.C. 
Tong, J.C.
Chai, C.L.L. 
Keywords: B-cell lymphoma-extra large (Bcl-XL)
Docking studies
Drug design
Myeloid cell leukemia sequence 1 (Mcl-1)
Issue Date: 2011
Citation: Bernardo, P.H., Sivaraman, T., Wan, K.-F., Xu, J., Krishnamoorthy, J., Song, C.M., Tian, L., Chin, J.S.F., Lim, D.S.W., Mok, H.Y.K., Yu, V.C., Tong, J.C., Chai, C.L.L. (2011). Synthesis of a rhodanine-based compound library targeting Bcl-XL and Mcl-1. Pure and Applied Chemistry 83 (3) : 723-731. ScholarBank@NUS Repository.
Abstract: 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. © 2011 IUPAC.
Source Title: Pure and Applied Chemistry
ISSN: 00334545
DOI: 10.1351/PAC-CON-10-10-29
Appears in Collections:Staff Publications

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