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Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors
Xingrui He1, Yuan Gao2, Zi Hui3
1Key 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.
Abstract:
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 IC50 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.
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