Synthesis and Evaluation of 2-Alkylthio-4-(N-substituted sulfonamide)pyrimidine Hydroxamic Acids as Anti-myeloma Agents
Synthesis and Evaluation of 2-Alkylthio-4-(N-substituted sulfonamide)pyrimidine Hydroxamic Acids as Anti-myeloma Agents
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DOI：
10.1111/cbdd.12678
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发表时间：
2016-03-01
影响因子：
3
通讯作者：
Bai, Xu
中科院分区：
文献类型：
--
作者：
Xiang, Jinbao;Leung, Crystal;Bai, Xu
合成了一系列嘧啶异羟肟酸类化合物，它们在第二位上具有硫醚取代基，在第四位上具有磺酰胺取代基，并评价了它们对人骨髓瘤细胞系RPMI 8226的活性。几种化合物显示出显著的抗癌效力。发现代表性化合物6a选择性地杀死癌细胞，但不杀死正常细胞。此外，化合物6a可有效地引起RPMI 8226细胞的凋亡，并表现出有希望的HDAC抑制活性。
A series of pyrimidine hydroxamic acids with a sulfide substituent at the second position and a sulfonamide substituent at the fourth position have been synthesized and evaluated for their activity against human myeloma cell line RPMI 8226. Several compounds exhibited significant anti-cancer potency. It was found that representative compound 6a selectively killed cancerous but not normal cells. Moreover, compound 6a was effective in causing apoptosis in RPMI 8226 cells and exhibited promising HDAC-inhibitory activities.