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https://dspace.ctu.edu.vn/jspui/handle/123456789/54720
Title: | Tổng hợp và thử hoạt tính sinh học của một số dẫn chất benzamid có nhân quinazolin |
Authors: | Nguyễn, Thị Thuận Nguyễn, Hải Nam Đoàn, Thanh Hiếu |
Keywords: | HDAC Histon deacetylase Acid hydroxamic |
Issue Date: | 2018 |
Series/Report no.: | Tạp chí Dược học;Số 512 .- Tr.41-44 |
Abstract: | A series of 6 novel benzamid incorporating quinazoline heterocycles (4a-f) were synthesized as novel histone deacetylases Inhibitors. By bioevaluation, these quinazoline-based benzamide showed potent cytotoxicity against the following three human cancer cell lines: SW620 (colon), PC-3 (prostate) and NCI-H23 (lung), displaying the potency 5 - up to 10-fold higher than SAFIA (suberoylanilidehydroxamic acid, vorinostat). Also, these compounds were comparable to SAHA in inhibiting HDACs with IC₅₀ values within the sub-micromolar range. Of these, two compounds (4c) and (4f) were HDAC inhibitors even more potent than SAHA in Hela extract assay and expected to be promising anticancer drug candidates. |
URI: | https://dspace.ctu.edu.vn/jspui/handle/123456789/54720 |
ISSN: | 0866-7861 |
Appears in Collections: | Dược học |
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_file_ Restricted Access | 3.08 MB | Adobe PDF | ||
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