4-羟基-3-甲基苯并呋喃-2-甲酰腙类化合物作为新型 LSD1 抑制剂。
4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors.
机构信息
Key Laboratory of Elemene Class Anti-Cancer Chinese Medicine of Zhejiang Province, PR China; Engineering Laboratory of Development and Application of Traditional Chinese Medicine from Zhejiang Province, PR China; Holistic Integrative Pharmacy Institutes (HIPI), School of Medicine, Hangzhou Normal University, Hangzhou, Zhejiang, 311121, PR China; School of Pharmacy, School of Chemistry and Chemical Engineering, Liaocheng University, Liaocheng, Shandong, 252000, PR China.
Key Laboratory of Elemene Class Anti-Cancer Chinese Medicine of Zhejiang Province, PR China; School of Clinical Medicine, Guangdong Pharmaceutical University, Guangzhou, Guangdong, 510000, PR China.
出版信息
Bioorg Med Chem Lett. 2020 May 15;30(10):127109. doi: 10.1016/j.bmcl.2020.127109. Epub 2020 Mar 13.
Histone lysine specific demethylase 1 (LSD1 or KDM1A) is a potential therapeutic target in oncology due to its overexpression in various human tumors. We report herein a new class of benzofuran acylhydrazones as potent LSD1 inhibitors. Among the 31 compounds prepared, 14 compounds exhibited excellent LSD1 inhibitory activity with IC values ranging from 7.2 to 68.8 nM. In cellular assays, several compounds inhibited the proliferations of various cancer cell lines, including PC-3, MCG-803, U87 MG, PANC-1, HT-29 and MCF-7. This opens up the opportunity for further optimization and investigation of this class compounds for potential cancer treatment.
组蛋白赖氨酸特异性去甲基酶 1（LSD1 或 KDM1A）在肿瘤学中是一个有潜力的治疗靶点，因为它在各种人类肿瘤中过度表达。我们在此报告了一类新的苯并呋喃酰腙作为有效的 LSD1 抑制剂。在所制备的 31 种化合物中，有 14 种化合物表现出优异的 LSD1 抑制活性，IC 值范围为 7.2 至 68.8 nM。在细胞实验中，几种化合物抑制了包括 PC-3、MCG-803、U87 MG、PANC-1、HT-29 和 MCF-7 在内的多种癌细胞系的增殖。这为进一步优化和研究这类化合物用于潜在的癌症治疗开辟了机会。
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