Page 51 - 《中国药科大学学报》2026年第1期
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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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