title: Novel indoline-1- or 3,4-dihydroquinoline-1(2H)-substituted carbothiohydrazides as TPO receptor agonists.
abstract: Synthesis and evaluation of novel series of indoline-1- or 3,4-dihydroquinoline-1(2H)-substituted carbothiohydrazide or carbohydrazide based small molecule compounds as thrombopoietin (TPO) receptor agonists are reported. Members of these compounds have been identified as full agonists of human c-mpl in BaF3/TPOR cell line. Indoline-1-carbohydrazide 9b exhibited reasonable pharmacokinetic profile.
authors.affiliation: Shanghai Hengrui Pharmaceuticals Co, Ltd, 279 Wenjing Rd, Shanghai 200245, China. tangpc@shhrp.com
authors.forename: Peng Cho
authors.initials: PC
authors.lastname: Tang
authors.forename: He Jun
authors.initials: HJ
authors.lastname: Lu
authors.forename: Yi Qian
authors.initials: YQ
authors.lastname: Chen
authors.forename: Hao
authors.initials: H
authors.lastname: Zheng
authors.forename: Peng
authors.initials: P
authors.lastname: Song
authors.forename: Li
authors.initials: L
authors.lastname: Wang
authors.forename: Qiang
authors.initials: Q
authors.lastname: Qin
authors.forename: Ai Shen
authors.initials: AS
authors.lastname: Gong
mesh_terms: D000818:Animals; D002460:Cell Line; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D011804:Quinolines / Q000737:chemistry*; D051381:Rats; D053628:Receptors, Thrombopoietin / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D006834:Hydrazines; D007211:Indoles; D011804:Quinolines; D053628:Receptors, Thrombopoietin; C082218:MPL protein, human; C057812:indoline; C037219:quinoline; C019289:carbohydrazide