Rational design, synthesis and biological evaluation of benzo [d] isoxazole derivatives as potent BET bivalent inhibitors for potential treatment of prostate cancer
J Li, R Zhu, X Zhuang, C Zhang, H Shen, X Wu… - Bioorganic …, 2023 - Elsevier
Multivalency is an attractive strategy for effective binding to target protein. Bromodomain and
extra-terminal (BET) family features two tandem bromodomains (BD1, BD2), which are …
extra-terminal (BET) family features two tandem bromodomains (BD1, BD2), which are …
Y06014 is a selective BET inhibitor for the treatment of prostate cancer
T Wu, Q Xiang, C Wang, C Wu, C Zhang… - Acta Pharmacologica …, 2021 - nature.com
Bromodomain and extra-terminal proteins (BETs) are potential targets for the therapeutic
treatment of prostate cancer (PC). Herein, we report the design, the synthesis, and a …
treatment of prostate cancer (PC). Herein, we report the design, the synthesis, and a …
Y08060: a selective BET inhibitor for treatment of prostate cancer
Q Xiang, Y Zhang, J Li, X Xue, C Wang… - ACS medicinal …, 2018 - ACS Publications
Prostate 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 …
deaths. The bromodomain and extra terminal domain (BET) family proteins have emerged …
Structure-Based Discovery and Optimization of Benzo[d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant …
M Zhang, Y Zhang, M Song, X Xue… - Journal of medicinal …, 2018 - ACS Publications
The bromodomain and extra-terminal (BET) family proteins have gained increasing interest
as drug targets for treatment of castration-resistant prostate cancer (CRPC). Here, we …
as drug targets for treatment of castration-resistant prostate cancer (CRPC). Here, we …
Discovery of BET specific bromodomain inhibitors with a novel scaffold
N Pandit, M Yoo, TH Park, J Kim, SM Kim… - Bioorganic & Medicinal …, 2022 - Elsevier
Bromodomain and extra-terminal domain (BET) proteins have been considered as potent
candidates for anti-cancer drug development. As epigenetic readers, they modulate gene …
candidates for anti-cancer drug development. As epigenetic readers, they modulate gene …
Benzoxazinone-containing 3, 5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer
X Xue, Y Zhang, C Wang, M Zhang, Q Xiang… - European Journal of …, 2018 - Elsevier
The bromodomain and extra-terminal proteins (BET) have emerged as promising
therapeutic targets for the treatment of castration-resistant prostate cancer (CRPC). We …
therapeutic targets for the treatment of castration-resistant prostate cancer (CRPC). We …
Exploiting the 7-methylimidazo [1, 5-a] pyrazin-8 (7H)-one scaffold for the development of novel chemical inhibitors for Bromodomain and Extraterminal Domain (BET) …
Y Yang, P Chen, L Zhao, F Zhang, B Zhang, C Xu… - Bioorganic …, 2019 - Elsevier
The bromodomain and extraterminal (BET) family of proteins play a crucial role in promoting
gene expression of critical oncogenes. Novel BET bromodomain inhibitors with excellent …
gene expression of critical oncogenes. Novel BET bromodomain inhibitors with excellent …
Novel phenanthridin-6 (5H)-one derivatives as potent and selective BET bromodomain inhibitors: Rational design, synthesis and biological evaluation
Y Zhi, S Wang, W Huang, S Zeng, M Liang… - European Journal of …, 2019 - Elsevier
Inhibition of BET family of bromodomain is an appealing intervention strategy for several
cancers and inflammatory diseases. This article highlights our work toward the identification …
cancers and inflammatory diseases. This article highlights our work toward the identification …
Design and development of a novel series of oral bivalent BET inhibitors with potent anticancer activities
M Luo, Q Wu, Y Yang, L Sun, X Huan, C Tian… - European Journal of …, 2022 - Elsevier
Bromodomain and extraterminal domain (BET) subfamily members are intriguing targets for
cancer treatment. Most of the reported BET inhibitors were monovalent inhibitors. Recently …
cancer treatment. Most of the reported BET inhibitors were monovalent inhibitors. Recently …
Discovery of Novel Inhibitors of BRD4 for Treating Prostate Cancer: A Comprehensive Case Study for Considering Water Networks in Virtual Screening and Drug …
H Zhong, X Wang, S Chen, Z Wang… - Journal of Medicinal …, 2023 - ACS Publications
Androgen receptor (AR) is the primary target for treating prostate cancer (PCa), which
inevitably progresses due to drug-resistant mutations. Bromodomain-containing protein 4 …
inevitably progresses due to drug-resistant mutations. Bromodomain-containing protein 4 …
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