Novel indoline-1- or 3,4-dihydroquinoline-1(2H)-substituted carbothiohydrazides as TPO receptor agonists.
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.
Tang
Peng Cho
PC
Shanghai Hengrui Pharmaceuticals Co, Ltd, 279 Wenjing Rd, Shanghai 200245, China. tangpc@shhrp.com
Lu
He Jun
HJ
Chen
Yi Qian
YQ
Zheng
Hao
H
Song
Peng
P
Wang
Li
L
Qin
Qiang
Q
Gong
Ai Shen
AS
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
D006834:Hydrazines; D007211:Indoles; D011804:Quinolines; D053628:Receptors, Thrombopoietin; C082218:MPL protein, human; C057812:indoline; C037219:quinoline; C019289:carbohydrazide