144464-66-4Relevant articles and documents
Asymmetric synthesis of tricyclic tetralin derivatives via an intramolecular photoreaction
Yang, Chao,Xia, Wu Jiong,Scheffer, John R.
, p. 6791 - 6795 (2007)
An intramolecular photoreaction for the synthesis of tricyclic tetralin derivatives through a Norrish/Yang type cyclization is described. Asymmetric studies on this reaction using ionic chiral auxiliaries gave enantiomeric excesses of up to 99% at conversions?of?80%, and the reaction mechanism was mapped out by a single crystal-to-single crystal reaction.
Design, synthesis, and biological evaluation of Cyclobentinib (CB1107) as a potential anti-CML agent
Zhou, Zijun,Wang, Yang,Li, Jun,Hu, Baichun,Lin, Xiaolin,Chen, Ye,Wang, Rui,Liu, Ju,Liu, Hongsheng
, p. 1863 - 1875 (2018/06/20)
Cyclobentinib was designed and synthesized as a novel anti-CML agent, its in vitro activity against K562 cells was evaluated by MTT assay. CB1107 showed remarkable cytotoxicity against K562 cell line with an IC50 of 0.037 ± 0.028 μmol/L, and thus it was 17-fold more potent than the reference drug Imatinib. Inducing cell apoptosis and affecting cell cycling of this compound in K562 cells were estimated by using flow cytometry and Acridine Orange/Ethidium Bromide (AO/EB) staining. The results showed that CB1107 was capable of arresting cell cycle at G0/G1 phase as well as inducing cell apoptosis significantly. Molecular mechanism of CB1107 was detected by the protein expression of Bcr-AblP210 using western blotting analysis. Downregulation of expression of Bcr-AblP210 was obviously revealed in the treatment of this tetralin amide compound. Of note, the results of these investigations suggested that CB1107 is more potent than the reference drug Imatinib against K562 cells. Additionally, in vivo results indicated that CB1107 significantly decreased tumor growth in K562 tumor-bearing Non-obese Diabetic/Severe Combined Immunodeficiency (NOD/SCID) mice. Histopathological investigation revealed that CB1107 without notable toxicity in a given dose range. These findings collectively demonstrate CB1107 is a promising candidate as a novel anti-CML agent.
F- Nucleophilic-Addition-Induced Allylic Alkylation
Tian, Panpan,Wang, Cheng-Qiang,Cai, Sai-Hu,Song, Shengjin,Ye, Lu,Feng, Chao,Loh, Teck-Peng
supporting information, p. 15869 - 15872 (2016/12/23)
Herein we present a novel strategy based on palladium-catalyzed allylic alkylation by taking advantage of the nucleophilic addition of external fluoride onto gem-difluoroalkenes as the initiation step. The merit of this protocol is highly appealing, as it enables a formal allylation of trifluoroethylarene derivatives through the in situ generation of β-trifluorocarbanions, which otherwise are deemed to be problematic in deprotonative allylation. Furthermore, this strategy distinguishes itself by high modularity, operational simplicity, and wide substrate scope with respect to allyl carbonates, giving rise to a broad array of homoallyltrifluoromethane derivatives, which otherwise would not be easily obtained using existing synthetic methods.
