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

Please use this identifier to cite or link to this item: https://doi.org/10.1351/PAC-CON-10-10-29

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) Rhodanine
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. https://doi.org/10.1351/PAC-CON-10-10-29
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
URI:	http://scholarbank.nus.edu.sg/handle/10635/101801
ISSN:	00334545
DOI:	10.1351/PAC-CON-10-10-29
Appears in Collections:	Staff Publications

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