{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["8(3)"],"submitter":["Shi Y"],"pubmed_abstract":["Herein we describe the design, synthesis, and biological evaluation of a novel series of tranylcypromine-based LSD1 inhibitors <i>via</i> 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 (<i>e.g.</i>14a, 15b, 16a, 19a and 20b) against closely related enzymes such as MAO-A, MAO-B, and LSD2."],"journal":["RSC advances"],"pagination":["1666-1676"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9077246"],"repository":["biostudies-literature"],"pubmed_title":["Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors."],"pmcid":["PMC9077246"],"pubmed_authors":["Gunosewoyo H","Tang J","Li J","Wu YR","Su MB","Yu LF","Shen DH","Yang F","Shi Y","Zhou YB"],"additional_accession":[]},"is_claimable":false,"name":"Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors.","description":"Herein we describe the design, synthesis, and biological evaluation of a novel series of tranylcypromine-based LSD1 inhibitors <i>via</i> 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 (<i>e.g.</i>14a, 15b, 16a, 19a and 20b) against closely related enzymes such as MAO-A, MAO-B, and LSD2.","dates":{"release":"2018-01-01T00:00:00Z","publication":"2018 Jan","modification":"2025-06-01T02:43:56.444Z","creation":"2025-06-01T02:43:56.444Z"},"accession":"S-EPMC9077246","cross_references":{"pubmed":["35540911"],"doi":["10.1039/c7ra13097j"]}}