214470-57-2Relevant articles and documents
Design, synthesis, docking and antitumor activity of quinazolino [3, 4-a] thieno [3, 2-d] pyrimidin-8-one derivatives
Zheng, Youguang,Wu, Xiaoqing,Xue, Bai,Li, Mingdong,Ji, Min
, p. 285 - 290 (2010)
Several novel quinazolino [3, 4-a] thieno [3, 2-d] pyrimidin-8-one derivatives were synthesized. All of the compounds were determined against MiaPaCa2 and DU145 cells in vitro, and the crystal structures of analog 8 and 20 in the active site of the EGFR c
Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment
Zhu, Jun,Wang, Li-Ning,Cai, Rong,Geng, Shang-Qi,Dong, Ya-Fei,Liu, Yu-Ming
, p. 1325 - 1329 (2019/04/08)
Dual binding site acetylcholinesterase (AChE) inhibitors and butyrylcholinesterase (BChE) inhibitors have recently emerged as two classes of new anti-Alzheimer agents to positively modify the disease's course. In this work, a new series of 4-N-phenylaminoquinolines was synthesized and evaluated for their abilities to inhibit AChE and BChE. Compound 11b showed significant inhibitory activities on AChE and BChE with IC50 values of 0.86 and 2.65 μM, respectively, a lot better than that of reference drug galanthamine. Furthermore, docking study showed that compound 11b interacted simultaneously not only with active and peripheral sites of AChE, but also with all five regions of BChE active site. These findings suggest that these derivatives could be regarded as promising starting points for further drug discovery developments.
1,3-disubstituted urea and thiourea derivative and application thereof
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Paragraph 0108; 0112-0114, (2019/01/23)
The invention discloses a 1,3-disubstituted urea and thiourea derivative and application thereof in the field of pharmaceutical chemistry. A structural formula of the derivative is as shown in the specification, and the derivative gives play to an antitumor function through inhibition of tyrosine protein kinase activity, wherein main tyrosine protein kinase inhibited by the derivative includes c-Met, IGF-1R, Src, c-Kit and the like. The derivative can be used for preparation of medicines for preventing or treating hyperplastic diseases, lung cancers, liver cancers, gastric cancers, colon cancers and breast cancers.