LSD1/KDM1A inhibitors in clinical trials: advances and prospects

Y Fang, G Liao, B Yu - Journal of hematology & oncology, 2019 - Springer
Histone demethylase LSD1 plays key roles during carcinogenesis, targeting LSD1 is
becoming an emerging option for the treatment of cancers. Numerous LSD1 inhibitors have …

FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application

S Wang, XH Yuan, SQ Wang, W Zhao, XB Chen… - European Journal of …, 2021 - Elsevier
Considerable progress has been made in the development of anticancer agents over the
past few decades, and a lot of new anticancer agents from natural and synthetic sources …

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

B Noce, E Di Bello, R Fioravanti, A Mai - Frontiers in pharmacology, 2023 - frontiersin.org
Histone lysine-specific demethylase 1 (LSD1/KDM1A) was first identified in 2004 as an
epigenetic enzyme able to demethylate specific lysine residues of histone H3, namely …

Triazole-fused pyrimidines in target-based anticancer drug discovery

XJ Dai, LP Xue, SK Ji, Y Zhou, Y Gao, YC Zheng… - European Journal of …, 2023 - Elsevier
In recent decades, the development of targeted drugs has featured prominently in the
treatment of cancer, which is among the major causes of mortality globally. Triazole-fused …

[HTML][HTML] Natural products as LSD1 inhibitors for cancer therapy

Y Fang, C Yang, Z Yu, X Li, Q Mu, G Liao… - Acta Pharmaceutica Sinica …, 2021 - Elsevier
Natural products generally fall into the biologically relevant chemical space and always
possess novel biological activities, thus making them a rich source of lead compounds for …

Reversible lysine specific demethylase 1 (LSD1) inhibitors: a promising wrench to impair LSD1

XJ Dai, Y Liu, LP Xue, XP Xiong, Y Zhou… - Journal of medicinal …, 2021 - ACS Publications
As a flavin adenine dinucleotide (FAD)-dependent monoamine oxidase, lysine specific
demethylase 1 (LSD1/KDM1A) functions as a transcription coactivator or corepressor to …

Catalytic Enantioselective Aminative Difunctionalization of Alkenes

N Huang, J Luo, L Liao, X Zhao - Journal of the American …, 2024 - ACS Publications
Enantioselective difunctionalization of alkenes offers a straightforward means for the rapid
construction of enantioenriched complex molecules. Despite the tremendous efforts devoted …

Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors

X Zhang, H Huang, Z Zhang, J Yan, T Wu, W Yin… - European Journal of …, 2021 - Elsevier
Abstract Lysine-specific demethylase 1 (LSD1) is a FAD-dependent enzyme, which has
been proposed as a promising target for therapeutic cancer. Herein, a series of benzofuran …

Installation of pargyline, a LSD1 inhibitor, in the HDAC inhibitory template culminated in the identification of a tractable antiprostate cancer agent

R Ojha, IC Chen, CM Hsieh, K Nepali… - Journal of Medicinal …, 2021 - ACS Publications
Pragmatic insertion of pargyline, a LSD1 inhibitor, as a surface recognition part in the HDAC
inhibitory pharmacophore was planned in pursuit of furnishing potent antiprostate cancer …

Intermolecular Hydrazinative Halogenation of Alkenes with Potassium Halides as Nucleophilic Halogen Sources: Modular Entry to Phenelzine Derivatives

N Huang, L Liao, X Zhao - Organic Letters, 2023 - ACS Publications
An approach for the efficient synthesis of halogenated hydrazines via acid-mediated
electrophilic hydrazinative halogenation of alkenes is disclosed. This transformation …