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1. Design, synthesis, and biological evaluation of novel carbazole derivatives as potent DNMT1 inhibitors with reasonable PK properties

Author

Ennian, Li, Kai, Wang, Bei, Zhang, Siqi, Guo, Senhao, Xiao, Qi, Pan, Xiaowan, Wang, Weiying, Chen, Yunshan, Wu, Hesong, Xu, Xiangqian, Kong, Cheng, Luo, Shijie, Chen, and Bo, Liu

Subjects
Mammals, Pharmacology, Carbazoles, Antineoplastic Agents, General Medicine, DNA Methylation, Cell Line, Tumor, Neoplasms, Drug Discovery, Animals, Humans, DNA (Cytosine-5-)-Methyltransferases, DNA Modification Methylases, Cell Proliferation
Abstract

The DNA methyltransferases (DNMTs) were found in mammals to maintain DNA methylation. Among them, DNMT1 was the first identified, and it is an attractive target for tumour chemotherapy. DC_05 and DC_517 have been reported in our previous work, which is non-nucleoside DNMT1 inhibitor with low micromolar IC

Published
2022

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