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dc.contributor.authorShi, Y.
dc.contributor.authorWu, Y.
dc.contributor.authorSu, M.
dc.contributor.authorShen, D.
dc.contributor.authorGunosewoyo, Hendra
dc.contributor.authorYang, F.
dc.contributor.authorLi, J.
dc.contributor.authorTang, J.
dc.contributor.authorZhou, Y.
dc.contributor.authorYu, L.
dc.identifier.citationShi, Y. and Wu, Y. and Su, M. and Shen, D. and Gunosewoyo, H. and Yang, F. and Li, J. et al. 2018. Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors. RSC Advances. 8 (3): pp. 1666-1676.

© The Royal Society of Chemistry 2018. Herein we describe the design, synthesis, and biological evaluation of a novel series of tranylcypromine-based LSD1 inhibitors via conformational restriction using spiro ring systems. A simple, direct spirocyclic analog of tranylcypromine (compounds 8a and 8b) was shown to be a 28- to 129-fold more potent inhibitor of LSD1 enzyme compared to tranylcypromine. Further incorporation of various substituted benzyl groups to the amino group resulted in a suite of 2',3'-dihydrospiro[cyclopropane-1,1'-inden]-2-amines that are potent LSD1 inhibitors with excellent selectivity profiles (e.g.14a, 15b, 16a, 19a and 20b) against closely related enzymes such as MAO-A, MAO-B, and LSD2.

dc.publisherRoyal Society of Chemistry
dc.titleNovel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors
dc.typeJournal Article
dcterms.source.titleRSC Advances
curtin.departmentSchool of Pharmacy and Biomedical Sciences
curtin.accessStatusOpen access

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