179688-29-0Relevant 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.
Catalytic cyclization preparation method and application of erlotinib key intermediate
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Paragraph 0022; 0033-0042, (2021/11/06)
The invention relates to a catalytic cyclization preparation method and application of an erlotinib key intermediate. By using 2-nitro-4, 5-bis (2-methoxyethoxy) ethyl benzoate as a raw material and adopting a polysaccharide-loaded nano-palladium catalyst, the erlotinib key intermediate 6, 7-bis (2-methoxyethoxy)-4-quinazolinone is prepared through a one-pot method. The erlotinib key intermediate is applied to preparation of quinazoline ring compounds. The method is carried out by adopting a catalytic one-pot method, the catalyst can be recycled for more than 10 times, the post-treatment is simple, the product purity is high, the next reaction can be directly carried out, the operation is simple, the pollution is less, and the cost is low. The method solves the problems of high catalyst price, high separation difficulty, high metal residue, more reaction three wastes and the like in the original process, greatly reduces the cost, provides technical guarantee for development of an industrial production process of erlotinib, and also provides a new reference method for synthesis of other anti-tumor drugs with quinazoline structures.
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
