79560-19-3Relevant articles and documents
Discovery of sertraline and its derivatives able to combat drug-resistant gastric cancer cell via inducing apoptosis
Mu, Chao,Peng, Rui-Kun,Guo, Chun-Ling,Li, Ao,Yang, Xiu-Ming,Zeng, Rong,Li, Yu-Long,Gu, Jing,Ouyang, Qin
supporting information, (2021/04/12)
Resistance phenomena during chemotherapy of tumor has been severely hampering the applications of chemotherapeutics. Due to advantage of drug repurposing, discovery of new chemosensitizers based on approved drugs is an effect strategy to find new candidates. Herein, we found antidepressant drug – sertraline, could sensitize drug-resistant gastric cancer cell (SGC-7901/DDP) with the IC50 value of 18.73 μM. To understand the structure–activity relationship and improve the activity, 30 derivatives were synthesized and evaluated. The IC50 value of the best compound was improved to 5.2 μM. Moreover, we found apoptosis induction and cell cycle arrest was the reason for the cell death of the drug-resistant cells after treatment of sertraline and derivatives, and PI3K/Akt/mTOR pathway was involved.
Titanium(IV)-Mediated Ring-Opening/Dehydroxylative Cross-Coupling of Diaryl-Substituted Methanols with Cyclopropanol Derivatives
Zhang, Si-Xuan,Ding, Yan,Wang, Jun-Jie,Shen, Chuanji,Zhou, Xiaocong,Chu, Xue-Qiang,Ma, Mengtao,Shen, Zhi-Liang
, p. 15753 - 15760 (2021/10/25)
A titanium(IV)-mediated ring-opening/dehydroxylative cross-coupling of diaryl-substituted methanols with a cyclopropanol derivative was developed. The reactions proceeded efficiently to provide synthetically useful γ,γ-diaryl esters in moderate to good yields, which could be applied to the functionalization of complex molecules derived from bioactive fenofibrate and isoxepac and the synthesis of a precursor of Zoloft.
Method for preparing serrine hydrochloride intermediate and impurities
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Paragraph 0033; 0034, (2020/12/31)
The invention relates to a method for preparing a sertraline hydrochloride intermediate and an impurity. The invention provides a method for refining 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone. The content of the impurity 4-(2,3-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone in the obtained product is less than 0.1%. The invention also relates to a method for preparing the isomer impurity 4-(2,3-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone from the mother solution.