DICP OpenIR
Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer
Xiang, Quping1,2; Zhang, Yan1,2; Li, Jiaguo1,3; Xue, Xiaoqian1,2; Wang, Chao1; Song, Ming1; Zhang, Cheng1,3; Wang, Rui1; Li, Chenchang1,3; Wu, Chun1; Zhou, Yulai3; Yang, Xiaohong3; Li, Guohui4; Ding, Ke5; Xu, Yong1
KeywordBromodomain Brd4 Prostate Cancer Epigenetics
Source PublicationACS MEDICINAL CHEMISTRY LETTERS
2018-03-01
ISSN1948-5875
DOI10.1021/acsmedchemlett.8b00003
Volume9Issue:3Pages:262-267
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS SubjectChemistry, Medicinal
WOS Research AreaPharmacology & Pharmacy
WOS KeywordINCREASED SURVIVAL ; BROMODOMAINS ; OPTIMIZATION ; ABIRATERONE ; CASTRATION ; STATISTICS ; RESISTANCE ; DISCOVERY
AbstractProstate cancer is a commonly diagnosed cancer and a leading cause of cancer-related deaths. The bromodomain and extra terminal domain (BET) family proteins have emerged as potential therapeutic targets for the treatment of castration resistant prostate cancer. A series of 2,2-dimethy1-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives were designed and synthesized as selective bromodomain containing protein 4 (BRD4) inhibitors. The compounds potently inhibit BRD4(1) with nanomolar IC50 values and exhibit high selectivity over most non-BET subfamily members. One of the representative compounds 36 (Y08060) effectively suppresses cell growth, colony formation, and expression of androgen receptor (AR), AR regulated genes, and MYC in prostate cancer cell lines. In in vivo studies, 36 demonstrates a good PK profile with high oral bioavailability (61.54%) and is a promising lead compound for further prostate cancer drug development.
Language英语
WOS IDWOS:000427331200017
PublisherAMER CHEMICAL SOC
Citation statistics
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/168891
Collection中国科学院大连化学物理研究所
Corresponding AuthorXu, Yong
Affiliation1.Guangzhou Med Univ, Chinese Acad Sci, Guangdong Prov Key Lab Biocomp, Joint Sch Life Sci,Guangzhou Inst Biomed & Hlth, Guangzhou, Guangdong, Peoples R China
2.Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 100049, Peoples R China
3.Jilin Univ, Sch Pharmaceut Sci, 1266 Fujin Rd, Changchun 130021, Jilin, Peoples R China
4.Chinese Acad Sci, Dalian Inst Chem Phys, State Key Lab Mol React Dynam, Lab Mol Modeling & Design, Dalian 116023, Liaoning, Peoples R China
5.Jinan Univ, Sch Pharm, 601 Huangpu Ave West, Guangzhou 510632, Guangdong, Peoples R China
Recommended Citation
GB/T 7714
Xiang, Quping,Zhang, Yan,Li, Jiaguo,et al. Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer[J]. ACS MEDICINAL CHEMISTRY LETTERS,2018,9(3):262-267.
APA Xiang, Quping.,Zhang, Yan.,Li, Jiaguo.,Xue, Xiaoqian.,Wang, Chao.,...&Xu, Yong.(2018).Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.ACS MEDICINAL CHEMISTRY LETTERS,9(3),262-267.
MLA Xiang, Quping,et al."Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer".ACS MEDICINAL CHEMISTRY LETTERS 9.3(2018):262-267.
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