Ring size changes in the development of class I HDAC inhibitors
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 HCT1...
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| Format: | Article |
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Taylor & Francis Group
2021-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
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| Online Access: | http://dx.doi.org/10.1080/14756366.2021.1941920 |
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doaj-d0c4b056f55e42ea84796c11c80521d02021-07-06T12:16:06ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742021-01-013611387140110.1080/14756366.2021.19419201941920Ring size changes in the development of class I HDAC inhibitorsEr-Chieh Cho0Chi-Yuan Liu1Di-Wei Tang2Hsueh-Yun Lee3School of Pharmacy, College of Pharmacy, Taipei Medical UniversitySchool of Pharmacy, College of Pharmacy, Taipei Medical UniversitySchool of Pharmacy, College of Pharmacy, Taipei Medical UniversitySchool of Pharmacy, College of Pharmacy, Taipei Medical UniversityFive 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.http://dx.doi.org/10.1080/14756366.2021.1941920thienylbenzamidesring transformationhdaccolon cancer |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Er-Chieh Cho Chi-Yuan Liu Di-Wei Tang Hsueh-Yun Lee |
| spellingShingle |
Er-Chieh Cho Chi-Yuan Liu Di-Wei Tang Hsueh-Yun Lee Ring size changes in the development of class I HDAC inhibitors Journal of Enzyme Inhibition and Medicinal Chemistry thienylbenzamides ring transformation hdac colon cancer |
| author_facet |
Er-Chieh Cho Chi-Yuan Liu Di-Wei Tang Hsueh-Yun Lee |
| author_sort |
Er-Chieh Cho |
| title |
Ring size changes in the development of class I HDAC inhibitors |
| title_short |
Ring size changes in the development of class I HDAC inhibitors |
| title_full |
Ring size changes in the development of class I HDAC inhibitors |
| title_fullStr |
Ring size changes in the development of class I HDAC inhibitors |
| title_full_unstemmed |
Ring size changes in the development of class I HDAC inhibitors |
| title_sort |
ring size changes in the development of class i hdac inhibitors |
| publisher |
Taylor & Francis Group |
| series |
Journal of Enzyme Inhibition and Medicinal Chemistry |
| issn |
1475-6366 1475-6374 |
| publishDate |
2021-01-01 |
| description |
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. |
| topic |
thienylbenzamides ring transformation hdac colon cancer |
| url |
http://dx.doi.org/10.1080/14756366.2021.1941920 |
| work_keys_str_mv |
AT erchiehcho ringsizechangesinthedevelopmentofclassihdacinhibitors AT chiyuanliu ringsizechangesinthedevelopmentofclassihdacinhibitors AT diweitang ringsizechangesinthedevelopmentofclassihdacinhibitors AT hsuehyunlee ringsizechangesinthedevelopmentofclassihdacinhibitors |
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1721317581681328128 |