- Design, synthesis and antitumor activity of icotinib derivatives
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EGFR-TK pathway is of high importance for the treatment of non-small-cell lung cancers (NSCLC), and it will be challenging to develop anti-tumor drugs that could inhibit both EGFR wild-type and mutant tumor cells. Here, a series of icotinib derivatives containing 1,2,3-triazole moiety were designed and synthesized through copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reactions. Preliminary CCK-8 assay showed that the prepared icotinib-1,2,3-triazole compounds such as a7 or a12 demonstrated potent in vitro antitumor activity against the NSCLC cells expressing both wild type EGFR and mutational EGFR. Further, the mechanism of action for compounds a7 and a12 induced NSCLC cells death was also detailed, and the results suggested a possible induced NSCLC cells death via inducing mitochondrial apoptosis and arresting cell cycle. Remarkably, the inhibition of EGFR by these icotinib derivatives was also studied. The results showed that compound a12 was a potent inhibitor for EGFR with IC50 value of 1.49 μM. Combining these results, an EGFR inhibitor a12 represents a promising new anti-NSCLC candidate that could induce apoptosis and arrest cell cycle.
- Mao, Longfei,Sun, Ge,Zhao, Jie,Xu, Guiqing,Yuan, Miaomiao,Li, Yue-Ming
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- Preparation method of erlotinib (by machine translation)
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2 -4 Difluoro 5 - 2 -dihydroquinazoline -4 ketone and a chlorination reagent are subjected to a condensation reaction in a solvent system; and the obtained 5 - [(6 ethynylphenyl) amino] 7 -3 difluoro quinazoline and diethylene glycol are subjected to an etherification reaction in a base reagent and a solvent system to obtain the erlotinib diecainide obtained by carrying out a cyclization 4 - reaction -4 - in an alkali reagent and a solvent system at a high temperature and carrying 4 - out -6 a 7 - cyclization reaction 3 - in a solvent system at a high temperature and carrying out a cyclization reaction in a 4 - solvent system 3 - at a high temperature.6 7 . The impurity is less and controllable, the next reaction can be directly carried out, the operation is simplified, the good yield can be obtained in each step, the process flow is simplified, and the safety and the environment protection are guaranteed. (by machine translation)
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- Quinolinamine compound with IDO1 inhibition function and preparation method thereof
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The invention discloses a quinolinamine compound with an IDO1 inhibition function and a preparation method of the quinolinamine compound, and belongs to the technical field of medicine synthesis. According to the technical scheme, triethylene glycol is us
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Paragraph 0044-0046
(2020/11/23)
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- Eck for nepal and hydrochloric acid eck for nepal preparation method and wherein intermediate
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The present invention relates to the technical field of medicine. Particularly provided are methods of preparing icotinib, icotinib hydrochloride, and intermediates thereof. The methods avoid the use of phosphoryl chloride, thereby greatly reducing the emission of pollutants, which is of major benefit to the economy and environment. Disclosed is a compound represented by formula A, B or C, wherein R1 and R2 are individually selected from methyl, ethyl, propyl or isopropyl, or R1 and R2 forms with a commonly bonded N atom to a 3- to 7-membered ring.
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- POLYMORPH FORMS OF ICOTINIB MALEATE AND USES THEREOF
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Provided are Icotinib maleate(the compound of Formula I) and polymorph forms thereof, and methods of preparing and using them.
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Page/Page column 10; 11
(2015/01/09)
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- POLYMORPHIC FORMS OF ICOTINIB AND USES THEREOF
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Provided are polymorphic forms of the compound of Formula I, preparation thereof and pharmaceutical compositions, and use of a polymorph above in the treatment of a disease, a disorder or a condition, or in the manufacturing of a medicament for the treatm
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Page/Page column 11; 12; 13
(2015/01/09)
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- METHODS OF PREPARING ICOTINIB AND ICOTINIB HYDROCHLORIDE, AND INTERMEDIATES THEREOF
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The present invention relates to the technical field of medicine. Provided are methods of preparing icotinib, icotinib hydrochloride, and intermediates thereof. The methods avoid the use of phosphoryl chloride, thereby greatly reducing the emission of pollutants, which is of major benefit to the economy and environment.
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- METHODS OF PREPARING ICOTINIB AND ICOTINIB HYDROCHLORIDE, AND INTERMEDIATES THEREOF
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The present invention relates to the technical field of medicine, and specifically provides methods for preparing Icotinib, Icotinib hydrochloride, and intermediates thereof. These methods avoid the use of phosphorus oxychloride, thereby greatly reducing the emission of pollutants, which is of major benefits to the economy and environment.
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- Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors
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Crown ether fused anilinoquinazoline analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities in an in vitro EGFR kinase assay a
- Hu, Shaojing,Xie, Guojian,Zhang, Don X.,Davis, Charles,Long, Wei,Hu, Yunyan,Wang, Fei,Kang, Xinshan,Tan, Fenlai,Ding, Lieming,Wang, Yinxiang
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p. 6301 - 6305
(2012/10/29)
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- NOVEL FUSED QUINAZOLINE DERIVATIVES USEFUL AS TYROSINE KINASE INHIBITORS
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Novel fused quinazoline compound having the structure, formula (I) pharmaceutical composition and method of use for treating tyrosine kinase-mediated disorders.
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Page/Page column 25-26
(2008/06/13)
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