62001-29-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel 4,4-difluoro-1-methyl-N, 6-diphenyl-5, 6-dihydro-4H-pyrimido [4, 5-b] [1, 2, 4] triazolo [4, 3-d] [1, 4] diazepin-8-amine derivatives as potential BRD4 inhibitors
Li, Jiuhui,Zhang, Wenjie,Qiu, Qianqian,Zhou, Daoguang,Feng, Ziying,Tong, Zhenzhen,Wei, Jiaxin,Huang, Wenlong,Li, Jieming,Qian, Hai,Shi, Wei
, p. 1117 - 1128 (2021)
Bromodomain-containing protein 4 (BRD4) plays an extremely important physiological role in cancer, and the BRD4 inhibitors can effectively inhibit the proliferation of tumor cells. By taking BI-2536 (PLK1 and BRD4 inhibitor) as the lead compound, sixteen
Linear Hydroaminoalkylation Products from Alkyl-Substituted Alkenes
Warsitz, Michael,Doye, Sven
supporting information, p. 15121 - 15125 (2020/10/23)
The regioselective conversion of alkyl-substituted alkenes into linear hydroaminoalkylation products represents a strongly desirable synthetic transformation. In particular, such conversions of N-methylamine derivatives are of great scientific interest, because they would give direct access to important amines with unbranched alkyl chains. Herein, we present a new one-pot procedure that includes an initial alkene hydroaminoalkylation with an α-silylated amine substrate and a subsequent protodesilylation reaction that delivers linear hydroaminoalkylation products with high selectivity from simple alkyl-substituted alkenes. For that purpose, new titanium catalysts have been developed, which are able to activate the α-C?H bond of more challenging α-silylated amine substrates. In addition, a direct relationship between the ligand structure of the new catalysts and the obtained regioselectivity is described.
RSK2 benzo triazole derivatives as inhibitors of synthesis and use
-
Paragraph 0075-0077, (2016/10/07)
The invention relates to synthesis of a benzotriazol derivative and its application, specifically to a compound as shown in the following formula II, a pharmaceutical composition containing the compound as shown in the formula II and an application of the compound in preparation of drugs for treating or preventing RSK2-mediated diseases.
Triazole and benzotriazole derivatives as novel inhibitors for p90 ribosomal S6 protein kinase 2: Synthesis, molecular docking and SAR analysis
Yuan, Jun,Zhong, Ye,Li, Shiliang,Zhao, Xue,Luan, Guoqin,Zhao, Zhenjiang,Huang, Jin,Li, Honglin,Xu, Yufang
, p. 1192 - 1198 (2013/10/21)
A series of triazole and benzotriazole derivatives as novel p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors were designed and synthesized. The in vitro activities against RSK2 were evaluated, and among 14 compounds, compounds 5, 6, 11, 12, 13 and 14 exhibited enzyme IC50 values of 8.91, 2.86, 3.19, 3.05, 4.49 and 2.09 μmol/L respectively. The proposed binding modes were simulated using molecular docking method, and the docking results coupled with the structure-activity relationship (SAR) analysis indicated that all these active compounds bound to the RSK2 ATP binding site at NTKD, and the electron-donating groups on the 4-position of phenyl were the determinant point for the inhibitory activity. In the present study, a series of triazole and benzotriazole derivatives as novel p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors were designed and synthesized. The in vitro activities of the 14 compounds against RSK2 were evaluated, among which, compounds 5, 6, 11, 12, 13 and 14 exhibited enzyme IC50 values of 8.91, 2.86, 3.19, 3.05, 4.49 and 2.09 μmol/L respectively. The proposed binding modes were simulated using molecular docking method, and the docking results coupled with the structure-activity relationship (SAR) analysis indicated that all our active compounds bound to the RSK2 ATP binding site at NTKD, and the electron-donating groups on the 4-position of phenyl were the key point for the inhibitory activity. Copyright
Simple and convenient preparation of 1-(arylamino)methylbenzotriazoles and -(arylamino)methylbenzimidazoles
Milata,Kada,Zalibera,Belicova
, p. 215 - 220 (2007/10/03)
The preparation of 1-(arylamino)methylbenzotriazoles 1a-17a and benzimidazoles 1b-17b is described and their antibacterial activity evaluated. 1-Hydroxymethylbenzazoles react with the appropriate aniline to yield the target compounds. These were characterized using 1H NMR, IR, UV spectra. The compounds displayed no significant antibacterial activity.
Substituent effects in the bis(benzotriazolylmethylation) of aromatic amines
Katritzky, Alan R.,Rachwal, Stanislaw,Wu, Jing
, p. 446 - 455 (2007/10/02)
1-(Hydroxymethyl)benzotriazole and aromatic amines react to give an equilibrium mixture of N-mono- and N,N-bis(benzotriazolylmethyl)arylamines.Electron-releasing substituents on the arylamine ring shift the equilibrium towards the N,N-bis(benzotriazolylme
