- Ring size changes in the development of class I HDAC inhibitors
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Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.
- Cho, Er-Chieh,Liu, Chi-Yuan,Tang, Di-Wei,Lee, Hsueh-Yun
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p. 1387 - 1401
(2021/07/06)
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- Diaminopyrimidine derivatives as growth hormone secrectgogue receptor (GHS-R) antagonists
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The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, obesity, and disorders associated with obesity such as noninsulin dependent diabetes mellitus.
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Page/Page column 48
(2010/02/13)
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