Design, Synthesis, and Evaluation of Benzoheterocyclic-Containing Derivatives as Novel HDAC1 Inhibitors
Abstract In this study, the synthesis and biological evaluation of a variety of benzoheterocyclic-containing benzamide derivatives were described. Some of these compounds were proved to inhibiting the activity of histone deacetylase 1 (HDAC1) with IC50 values below the micromolar range, retarding pr...
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| Format: | Book |
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Georg Thieme Verlag KG,
2022-03-01T00:00:00Z.
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| 001 | doaj_652a7f8b7fe445a4a95d61be96e99bb0 | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Min-Ru Jiao |e author |
| 700 | 1 | 0 | |a Bo Han |e author |
| 700 | 1 | 0 | |a Xiu Gu |e author |
| 700 | 1 | 0 | |a Hao Zhang |e author |
| 700 | 1 | 0 | |a Ai-Ping Wang |e author |
| 700 | 1 | 0 | |a Qing-Wei Zhang |e author |
| 245 | 0 | 0 | |a Design, Synthesis, and Evaluation of Benzoheterocyclic-Containing Derivatives as Novel HDAC1 Inhibitors |
| 260 | |b Georg Thieme Verlag KG, |c 2022-03-01T00:00:00Z. | ||
| 500 | |a 2628-5088 | ||
| 500 | |a 2628-5096 | ||
| 500 | |a 10.1055/s-0042-1743487 | ||
| 520 | |a Abstract In this study, the synthesis and biological evaluation of a variety of benzoheterocyclic-containing benzamide derivatives were described. Some of these compounds were proved to inhibiting the activity of histone deacetylase 1 (HDAC1) with IC50 values below the micromolar range, retarding proliferation of several human cancer cells, and surprisingly, not possessing toxicity to human normal cells and hERG K+ ion channels. Among those compounds, 3c was the most potent and efficacious derivative. Compound 3c was orally active and displayed excellent in vivo antitumor activity in a HCT-116 xenograft mice model. | ||
| 546 | |a EN | ||
| 690 | |a benzamide derivatives | ||
| 690 | |a hdac1 inhibitors | ||
| 690 | |a orally active | ||
| 690 | |a antitumor activity | ||
| 690 | |a Pharmacy and materia medica | ||
| 690 | |a RS1-441 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Pharmaceutical Fronts, Vol 04, Iss 01, Pp e22-e29 (2022) | |
| 787 | 0 | |n http://www.thieme-connect.de/DOI/DOI?10.1055/s-0042-1743487 | |
| 787 | 0 | |n https://doaj.org/toc/2628-5088 | |
| 787 | 0 | |n https://doaj.org/toc/2628-5096 | |
| 856 | 4 | 1 | |u https://doaj.org/article/652a7f8b7fe445a4a95d61be96e99bb0 |z Connect to this object online. |