title: Synthesis and biological evaluation of a novel human stem/progenitor cells proliferation activator: 4-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl) thiosemicarbazide (Stemazole).
abstract: Stem/progenitor cells are crucial for cell-based therapy and regenerative medicine, and their application in clinical and basic research requires a large supply of cells. To identify effective stem/progenitor cell proliferation activators, we synthesised a series of new 4-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl) thiosemicarbazide (named Stemazole) derivatives. Preliminary evaluation of the structure-activity relationship (SAR) and the biological activities of the compounds were determined with a luminescent cell viability assay. The identified leading compound, Stemazole, exhibited remarkable proliferation-promoting activity in human hippocampal stem/progenitor cells (HSCs) in a time-dependent and concentration-dependent manner. The proliferation-promoting activity of Stemazole was further confirmed against a panel of human stem/progenitor cells derived from each of the three blastoderm layers. In conclusion, Stemazole is a novel activator of stem cells proliferation.
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Sun
authors.forename: Wei
authors.initials: W
authors.lastname: Wang
authors.forename: Yuanyuan
authors.initials: Y
authors.lastname: Sun
authors.forename: Mei
authors.initials: M
authors.lastname: Han
mesh_terms: D001756:Blastoderm / Q000166:cytology / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006624:Hippocampus / Q000166:cytology / Q000187:drug effects; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D008163:Luminescent Measurements; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D061251:Primary Cell Culture; D013234:Stem Cells / Q000166:cytology / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D006834:Hydrazines; D010069:Oxadiazoles; C559095:hydrazinecarbothioamide,N-(4-(4,5-dihydro-5-thioxo-1,3,4-oxadiazol-2-yl)phenyl)