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 36 compounds prepared, 15 compounds exhibited excellent LSD1 inhibitory activity with IC₅₀ values ranging from 3.5 to 89 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脱甲基酶1（LSD1或KDM1A）由于在各种人类肿瘤中的过表达而成为肿瘤学中的潜在治疗靶标。我们在此报告了一类新的苯并呋喃酰基hydr作为有效的LSD1抑制剂。在制备的36种化合物中，有15种化合物表现出出色的LSD1抑制活性，IC ₅₀值为3.5至89 nM。在细胞测定中，几种化合物抑制了各种癌细胞系的增殖，包括PC-3，MCG-803，U87 MG，PANC-1，HT-29和MCF-7。这为进一步优化和研究此类化合物用于潜在的癌症治疗提供了机会。