1609-06-9Relevant articles and documents
Application of heterocyclic thiol compound in preparation of antitumor drugs
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Paragraph 0043-0044, (2021/08/25)
The heterocyclic thiol compound provided by the invention shows good anti-hepatoma cells. Human breast cancer cells or human non-small cell lung cancer cell activity lays a foundation for screening and development of new drugs, and has good practical value.
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome
Zhou, Yu,Ma, Jing,Lin, Xingyu,Huang, Xi-Ping,Wu, Kaichun,Huang, Niu
, p. 707 - 720 (2016/02/09)
Here we employed structure-based ligand discovery techniques to explore a recently determined crystal structure of the 5-hydroxytryptamine 2B (5-HT2B) receptor. Ten compounds containing a novel chemical scaffold were identified; among them, seven molecules were active in cellular function assays with the most potent one exhibiting an IC50 value of 27.3 nM. We then systematically probed the binding characteristics of this scaffold by designing, synthesizing, and testing a series of structural modifications. The structure-activity relationship studies strongly support our predicted binding model. The binding profiling across a panel of 11 5-HT receptors indicated that these compounds are highly selective for the 5-HT2B receptor. Oral administration of compound 15 (30 mg/kg) produced significant attenuation of visceral hypersensitivity in a rat model of irritable bowel syndrome (IBS). We expect this novel scaffold will serve as the foundation for the development of 5-HT2B antagonists for the treatment of IBS.
Towards metformin prodrugs
Huttunen, Kristiina M.,Leppaenen, Jukka,Kemppainen, Eeva,Palonen, Piia,Rautio, Jarkko,Jaervinen, Tomi,Vepsaelaeinen, Jouko
scheme or table, p. 3619 - 3624 (2009/07/04)
The first examples of possible metformin prodrugs have been synthesized and characterized by spectroscopic methods. These five different types of chemically stable prodrugs were prepared from metformin and the corresponding halogenated promoieties. The products from unstable derivatives were also identified and reasons for the rearrangements are discussed. Georg Thieme Verlag Stuttgart · New York.