香豆素连接的4-苯胺甲基-1,2,3-三唑作为参与肿瘤发生的碳酸酐酶IX和XIII的有效抑制剂的合成及生物学评价
Synthesis and Biological Evaluation of Coumarin-Linked 4-Anilinomethyl-1,2,3-Triazoles as Potent Inhibitors of Carbonic Anhydrases IX and XIII Involved in Tumorigenesis.
作者信息
Thacker Pavitra S, Tiwari Prerna L, Angeli Andrea, Srikanth Danaboina, Swain Baijayantimala, Arifuddin Mohammed, Supuran Claudiu T
机构信息
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Balanagar, Hyderabad 500037, Telangana, India.
Neurofarba Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
出版信息
Metabolites. 2021 Apr 7;11(4):225. doi: 10.3390/metabo11040225.
A series of coumarin-linked 4-anilinomethyl-1,2,3-triazoles (-) was synthesized via a molecular hybridization approach, through carbon C-6 of the coumarin moiety. The synthesized compounds were evaluated for their inhibition of carbonic anhydrase (CA) isoforms I, II, IX and XIII. CAs IX and XIII were selectively inhibited over the off-target isoforms I and II. The best inhibitory profiles against CA IX were shown by compounds , and (K < 50 nM), with compound displaying the best inhibition with a K value of 36.3 nM. Compounds , , , and exhibited the best inhibitory profiles against CA XIII (K < 100 nM). These compounds can be further explored for the discovery of potent and effective CA IX and CA XIII inhibitors.
通过分子杂交方法，经由香豆素部分的碳C-6合成了一系列香豆素连接的4-苯胺甲基-1,2,3-三唑（-）。对合成的化合物进行了碳酸酐酶（CA）同工型I、II、IX和XIII抑制作用的评估。与脱靶同工型I和II相比，CA IX和XIII受到选择性抑制。化合物 、 和 对CA IX表现出最佳抑制谱（K<50 nM），其中化合物 的抑制效果最佳，K值为36.3 nM。化合物 、 、 、 和 对CA XIII表现出最佳抑制谱（K<100 nM）。这些化合物可进一步用于发现强效且有效的CA IX和CA XIII抑制剂。
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