CGK733(CGK733) - 药物靶点：ATM x ATR_专利_临床

概要

基本信息

药物类型

化学药

别名

靶点

ATM x ATR

作用机制

ATM抑制剂(丝氨酸蛋白激酶ATM抑制剂)、ATR抑制剂(丝氨酸蛋白激酶ATR抑制剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Korea Advanced Institute of Science & Technology

在研机构

Korea Advanced Institute of Science & Technology

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 CGK733 相关的临床结果

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100 项与 CGK733 相关的转化医学

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100 项与 CGK733 相关的专利（医药）

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1

项与 CGK733 相关的文献（医药）

2024-06-21·Bioscience, Biotechnology, and Biochemistry

Synthesis, growth inhibitory activity against tumor cells, and structure-activity relationship of CGK733 and its analogs

Article

作者: Katsuta, Ryo ; Kaida, Daisuke ; Wakamori, Shinnosuke ; Inagaki, Yuta ; Ishigami, Ken ; Yajima, Arata ; Hashimoto, Kohki

ABSTRACTCGK733 was reported as a compound that inhibited ATM/ATR kinase activities and blocked their checkpoint signaling pathways with great selectivity. However, this paper was subsequently retracted, and the truth about the activity of CGK733 remains unclear. We synthesized various analogs of CGK733 with a modification of the carboxylic acid moiety and/or the aniline derivative moiety to accumulate knowledge of the structure-activity relationship of this compound. Growth inhibitory activity of CGK733 and novel 35 analogs against HeLa S3 cells was evaluated, and the structure-activity relationship revealed that analogs with the 2-naphthyl or 4-fluorophenyl group instead of the benzhydryl group have activity comparable to CGK733 and that the 3-nitro group on the aniline moiety significantly affects the activity.

100 项与 CGK733 相关的药物交易

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