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Synthesis and biological evaluation of oxoindolin-3-ylidene ethyl benzothiohydrazides as non-peptide TPO mimics. 2010

Peng Cho Tang, and He Jun Lu, and Yi Qian Chen, and Sheng Lan Wang, and Hao Zheng, and Li Wang
Shanghai Hengrui Pharmaceuticals Co., Ltd, Shanghai, China. tangpc@shhrp.com

A novel series of oxoindolin-3-ylidene ethyl benzohydrazides were designed, synthesized, and identified as small molecule agonists of thrombopoietin (TPO) receptor c-mpl. Sulfur-oxygen exchange in oxoindolin-3-ylidene ethyl benzohydrazides was found to improve their agonistic activities. Several oxoindolin-3-ylidene ethyl benzothiohydrazides have been identified as full agonists of c-mpl.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D010455 Peptides Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are considered to be larger versions of peptides that can form into complex structures such as ENZYMES and RECEPTORS. Peptide,Polypeptide,Polypeptides
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D004353 Drug Evaluation, Preclinical Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications. Drug Screening,Evaluation Studies, Drug, Pre-Clinical,Drug Evaluation Studies, Preclinical,Drug Evaluations, Preclinical,Evaluation Studies, Drug, Preclinical,Evaluation, Preclinical Drug,Evaluations, Preclinical Drug,Medicinal Plants Testing, Preclinical,Preclinical Drug Evaluation,Preclinical Drug Evaluations,Drug Screenings,Screening, Drug,Screenings, Drug
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D053628 Receptors, Thrombopoietin Cell surface receptors that are specific for THROMBOPOIETIN. They contain two central FIBRONECTIN TYPE III DOMAINS and signal through interaction with JANUS KINASES such as JANUS KINASE 2. Antigens, CD110,CD110 Antigens,MPL Ligand Receptor,Thrombopoietin Receptor,Thrombopoietin Receptors
D018716 Molecular Mimicry The structure of one molecule that imitates or simulates the structure of a different molecule. Antigenic Mimicry,DNA Mimicry,Mimicry, Molecular,Antigen Mimicry,Antigen Mimicries,Antigenic Mimicries,DNA Mimicries,Mimicries, Antigen,Mimicries, Antigenic,Mimicries, DNA,Mimicries, Molecular,Mimicry, Antigen,Mimicry, Antigenic,Mimicry, DNA,Molecular Mimicries

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