1441640-67-0Relevant articles and documents
Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib
Li, Yong-Tao,Wang, Jing-Han,Pan, Cheng-Wen,Meng, Fan-Fei,Chu, Xiao-Qian,Ding, Ya-Hui,Qu, Wen-Zheng,Li, Hui-Ying,Yang, Cheng,Zhang, Quan,Bai, Cui-Gai,Chen, Yue
, p. 1419 - 1427 (2016)
Three novel series of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib were prepared and evaluated in vitro for their cytostatic effects against a human chronic myeloid leukemia (K562), acute myeloid leukemia (HL60), and human leukemia stem-like cell line (KG1a). The structure-activity relationship was analyzed by determining the inhibitory rate of each imatinib analog. Benzene and piperazine rings were necessary groups in these compounds for maintaining inhibitory activities against the K562 and HL60 cell lines. Introducing a trifluoromethyl group significantly enhanced the potency of the compounds against these two cell lines. Surprisingly, some compounds showed significant inhibitory activities against KG1a cells without inhibiting common leukemia cell lines (K562 and HL60). These findings suggest that these compounds are able to inhibit leukemia stem-like cells.
Heterocycle compound containing triazole, as well as preparation method and application of heterocycle compound
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Paragraph 0106; 0107; 0108; 0109; 0140; 0141; 0142, (2017/02/02)
The invention provides a heterocycle compound containing triazole, as well as a preparation method and application of the heterocycle compound. The heterocycle compound containing the triazole has a general formula in the following structure (as shown in
Safe and highly efficient syntheses of triazole drugs using Cu2O nanoparticle in aqueous solutions
Wang, Jing-Han,Pan, Cheng-Wen,Li, Yong-Tao,Meng, Fan-Fei,Zhou, Hong-Gang,Yang, Cheng,Zhang, Quan,Bai, Cui-Gai,Chen, Yue
, p. 3406 - 3409 (2013/07/19)
Triazole moiety is frequently employed in drug discovery and optimization. However, most syntheses of triazole drugs involve isolation of highly explosive azides. Herein we report safe and high efficient syntheses of triazole drugs in aqueous/organic solvent systems with Cu2O nanoparticle (Cu 2O-NP) as the catalyst of azide-alkyne cycloaddition (CuAAC). Since Cu2O-NP can be efficiently dispensed in aqueous and some organic solvents, the azide solutions from the previous preparation could be used directly in the next CuAAC stage without isolation. Therefore, this synthetic strategy is safe, convenient, and high yielding for the syntheses of triazole drugs.