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.
Nickel-Catalyzed α-Carbonylalkylarylation of Vinylarenes: Expedient Access to γ,γ-Diarylcarbonyl and Aryltetralone Derivatives
Dhungana, Roshan K.,Giri, Ramesh,Khanal, Namrata,Shekhar, K. C.
, p. 8047 - 8051 (2020/04/30)
We report a Ni-catalyzed regioselective α-carbonylalkylarylation of vinylarenes with α-halocarbonyl compounds and arylzinc reagents. The reaction works with primary, secondary, and tertiary α-halocarbonyl molecules, and electronically varied arylzinc reagents. The reaction generates γ,γ-diarylcarbonyl derivatives with α-secondary, tertiary, and quaternary carbon centers. The products can be readily converted to aryltetralones, including a precursor to Zoloft, an antidepressant drug.