{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Masagalli JN"],"funding":["National Research Foundation of Korea","Dongguk University"],"pagination":["1327"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC7958322"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["26(5)"],"pubmed_abstract":["Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key factor in several cardiovascular diseases, as it is responsible for the elevation of circulating low-density lipoprotein cholesterol (LDL-C) levels in blood plasma by direct interaction with the LDL receptor. The development of orally available drugs to inhibit this PCSK9-LDLR interaction is a highly desirable objective. Here, we report the synthesis of naturally occurring moracin compounds and their derivatives with a 2-arylbenzofuran motif to inhibit PCSK9 expression. In addition, we discuss a short approach involving the three-step synthesis of moracin C and a divergent method to obtain various analogs from one starting material. Among the tested derivatives, compound 7 (97.1%) was identified as a more potent inhibitor of PC"],"journal":["Molecules (Basel, Switzerland)"],"pubmed_title":["Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells."],"pmcid":["PMC7958322"],"funding_grant_id":["2018","NRF-2017R1D1A1B03036116"],"pubmed_authors":["Choi WJ","Masagalli JN","BasavanaGowda MK","Chae HS"],"additional_accession":[]},"is_claimable":false,"name":"Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells.","description":"Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key factor in several cardiovascular diseases, as it is responsible for the elevation of circulating low-density lipoprotein cholesterol (LDL-C) levels in blood plasma by direct interaction with the LDL receptor. The development of orally available drugs to inhibit this PCSK9-LDLR interaction is a highly desirable objective. Here, we report the synthesis of naturally occurring moracin compounds and their derivatives with a 2-arylbenzofuran motif to inhibit PCSK9 expression. In addition, we discuss a short approach involving the three-step synthesis of moracin C and a divergent method to obtain various analogs from one starting material. Among the tested derivatives, compound 7 (97.1%) was identified as a more potent inhibitor of PC","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Mar","modification":"2025-04-19T15:35:19.502Z","creation":"2021-03-18T08:34:53Z"},"accession":"S-EPMC7958322","cross_references":{"pubmed":["33801308"],"doi":["10.3390/molecules26051327"]}}