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第 57 卷第 1 期 邴天德,等:乳酸脱氢酶 A 抑制剂的设计、合成与生物活性 45
优的成药性。最后,对化合物 25 进行了体外细胞毒 substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of
human lactate dehydrogenase[J]. Bioorg Med Chem Lett, 2013,
性评价,其在胰腺癌细胞中显示出微摩尔级的抑制
23(11): 3186-3194.
活性(IC = 28.09 μmol/L),在正常细胞中显示出优 [13] Zhou Y, Tao PD, Wang MG, et al. Development of novel hu-
50
良的安全性。本研究为后续开发兼具优良成药性和 man lactate dehydrogenase A inhibitors: high-throughput
强效抑制活性的 LDHA 抑制剂奠定了实验基础。 screening, synthesis, and biological evaluations[J]. Eur J Med
Chem, 2019, 177: 105-115.
[14] Cox JH, Boily MO, Caron A, et al. Characterization of CHK-
336, a first-in-class, liver-targeted, small-molecule lactate dehy-
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