2148-55-2Relevant articles and documents
Discovery of quinazolinyl-containing benzamides derivatives as novel HDAC1 inhibitors with in vitro and in vivo antitumor activities
Zhang, Zixue,Zhang, Qingwei,Zhang, Hao,Jiao, Minru,Guo, Zheng,Peng, Xinyan,Fu, Lei,Li, Jianqi
, (2021/10/16)
A series of quinazolinyl-containing benzamide derivatives were designed, synthesized and evaluated for their in vitro histone deacetylase 1 (HDAC1) inhibitory activities. Compounds 11a surpassed the known class I selective HDAC inhibitor MS-275 in both HDAC1 enzymatic inhibitory activity and cellular anti-proliferative activity against a selected set of cancer cell types (Hut78, K562, Hep3B and HCT116 cells) with no observed effects on human normal cells. In particular, compound 11a inhibited HDAC1 over the other tested HDACs isoforms (HDAC2, HDAC6 and HDAC8) with acceptable safety profiles. Moreover, compound 11a displayed favorable oral pharmacokinetic properties and showed significant antitumor activity in the A549 tumor xenograft model in vivo.
4-aminoquinazoline grafted acrylamide compounds, preparation method and application thereof
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Paragraph 0070; 0071, (2020/01/12)
The invention relates to 4-aminoquinazoline grafted acrylamide compounds, a preparation method and application thereof. The compounds have a structure shown as general formula (I) in the specification. According to the invention, a quinazoline compound is adopted as the basis, and acrylamido is introduced into the system to synthesize a series of acrylamido-containing substituted 4-aminoquinazoline compounds, and the compounds have a good inhibiting effect on plant pathogenic bacteria, and have good inhibiting effect on pathogenic bacteria directed at Xanthomonas oryzae pv. Oryzae, Xanthomonasaxonopodis pv. Citri, etc.