183322-18-1Relevant 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-arylmercaptoquinazoline compound as well as preparation method and medical application thereof
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Paragraph 0024; 0026, (2021/01/24)
The invention discloses a 4-arylmercaptoquinazoline compound as well as a preparation method and medical application thereof. The 4-arylmercaptoquinazoline compound is reported for the first time. Research finds that the 4-arylmercaptoquinazoline compound has LSD1 inhibitory activity and has a prospect of being developed into antitumor drugs. Taking the compound 1 as an example, the IC50 value ofthe compound for inhibiting the LSD1 protein is 0.69 [mu]M and is remarkably superior to that of positive control; and in an anti-tumor test, the compound has relatively strong inhibitory activity ongastric cancer MGC-803, gastric cancer BGC-823, gastric cancer SGC-7901, breast cancer MCF-7, lung cancer H1650, lung cancer A549, lung cancer H1975, lung cancer H460, esophageal cancer EC-109, livercancer HepG2 and leukemia THP1 cells, and has a prospect of being developed into medicines for resisting gastric cancer, breast cancer, lung cancer, cancer of the esophagus, liver cancer and leukemia.
Transition-metal and oxidant-free approach for the synthesis of diverse N-heterocycles by TMSCl activation of isocyanides
Chen, Fen-Er,Dong, Lin,Li, Hongyan,Liu, Jinxin,Luo, Liangliang,Xiao, You-Cai,Zhou, Yuan
, p. 29257 - 29262 (2020/10/02)
A highly efficient TMSCl-mediated addition of N-nucleophiles to isocyanides has been achieved. This transition-metal and oxidant-free strategy has been applied to the construction of various N-heterocyles such as quinazolinone, benzimidazole and benzothiazole derivatives by the use of distinct amino-based binucleophiles. The notable feature of this protocol includes its mild reaction condition, broad functional group tolerance and excellent yield. This journal is