具有1,4-三唑部分的对称分子作为肿瘤相关乳酸脱氢酶-A的有效抑制剂。
Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A.
作者信息
Altamimi Abdul-Malek S, Alafeefy Ahmed M, Balode Agnese, Vozny Igor, Pustenko Aleksandrs, El Shikh Mohey Eldin, Alasmary Fatmah A S, Abdel-Gawad Sherif A, Žalubovskis Raivis
机构信息
a Department of Pharmaceutical Chemistry, College of Pharmacy , Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia.
b Department of Chemistry , Kulliyyah of Science, International Islamic University Malaysia.
出版信息
J Enzyme Inhib Med Chem. 2018 Dec;33(1):147-150. doi: 10.1080/14756366.2017.1404593.
A series of symmetric molecules incorporating aryl or pyridyl moieties as central core and 1,4-substituted triazoles as a side bridge was synthesised. The new compounds were investigated as lactate dehydro-genase (LDH, EC 1.1.1.27) inhibitors. The cancer associated LDHA isoform was inhibited with IC = 117-174 µM. Seven compounds exhibited better LDHA inhibition (IC 117-136 µM) compared to known LDH inhibitor - galloflavin (IC 157 µM).
合成了一系列以芳基或吡啶基部分为中心核、1,4-取代三唑为侧桥的对称分子。对这些新化合物作为乳酸脱氢酶（LDH，EC 1.1.1.27）抑制剂进行了研究。与癌症相关的LDHA同工型受到抑制，IC₅₀ = 117 - 174 μM。与已知的LDH抑制剂没食子黄素（IC₅₀ 157 μM）相比，七种化合物表现出更好的LDHA抑制作用（IC₅₀ 117 - 136 μM）。
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