Please use this identifier to cite or link to this item: http://scholarbank.nus.edu.sg/handle/10635/119811
Title: SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF RESORCYLIC ACID LACTONES AND DERIVATIVES AS PROTEIN KINASE INHIBITORS TARGETING TO CANCERS
Authors: XU JIN
Keywords: kinase inhibitor, resorcylic acid lactone, covalent, CDK, MNK, FLT3
Issue Date: 2-Jan-2015
Citation: XU JIN (2015-01-02). SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF RESORCYLIC ACID LACTONES AND DERIVATIVES AS PROTEIN KINASE INHIBITORS TARGETING TO CANCERS. ScholarBank@NUS Repository.
Abstract: RESORCYLIC ACID LACTONE (RAL) IS A CLASS OF MACROCYCLIC NATURAL PRODUCTS WHICH RECENTLY ATTRACTED THE ATTENTION OF BOTH ACADEMIA AND PHARMACEUTICAL COMPANIES DUE TO THEIR INTRIGUING BIOLOGICAL ATTRIBUTES. HERE, WE ARE INTERESTED IN THE CHEMISTRY AND THE BIOLOGICAL ACTIVITIES OF RALS AND DESIGNED ANALOGUES AGAINST CDK2, MNK1/2 AND FLT3 ET AL KINASES. OUR INITIAL STUDY IN RALS FOCUSED ON THE SYNTHESIS OF AIGIALOMYCIN D AND ITS ANALOGUES. WE ALSO REVEALED THAT THIS SERIES OF COMPOUNDS HAVE INTERESTING KINASE INHIBITORY ACTIVITIES AGAINST CDK2, MNK1/2 AND SOME OTHER KINASE TARGETS. WE EXTENDED THE SCOPE OF OUR STUDIES TO INCLUDE THE DESIGN AND SYNTHESIS OF COVALENT KINASE INHIBITORS BASED ON A NOVEL ENAMIDE RAL COMPOUNDS. LASTLY, WE DESCRIBED A RATIONAL DESIGN OF SOME SIMPLIFIED RING-OPENED RAL DERIVATIVES TARGETING THE FLT3 KINASES.
URI: http://scholarbank.nus.edu.sg/handle/10635/119811
Appears in Collections:Ph.D Theses (Open)

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