title: HIF-1α inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
abstract: The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.
authors.affiliation: College of Pharmacy, Dongguk University-Seoul, Seoul 100-715, South Korea.
authors.forename: Yan
authors.initials: Y
authors.lastname: Xia
authors.forename: Yinglan
authors.initials: Y
authors.lastname: Jin
authors.forename: Navneet
authors.initials: N
authors.lastname: Kaur
authors.forename: Yongseok
authors.initials: Y
authors.lastname: Choi
authors.forename: Kyeong
authors.initials: K
authors.lastname: Lee
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051795:Hypoxia-Inducible Factor 1, alpha Subunit / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D051795:Hypoxia-Inducible Factor 1, alpha Subunit; C540981:moracin O; C540980:moracin P