13365-26-9Relevant articles and documents
Designed, synthesized and biological evaluation of proteolysis targeting chimeras (PROTACs) as AR degraders for prostate cancer treatment
Ke, Yu,Liang, Jian-Jia,Liu, Hong-Min,Shan, Li-Hong,Wang, Ni,Wang, Ya-Lei,Wang, Zhi-Jia,Xie, Hang,Yang, Rui-Hua,Zheng, Zi-Jun,Zhou, Chen
, (2021)
As a continuation of our research on developing potent and potentially safe androgen receptor (AR) degrader, a series of novel proteolysis targeting chimeras (PROTACs) containing the phthalimide degrons with different linker were designed, synthesized and evaluated for their AR degradation activity against LNCaP (AR+) cell line. Most of the synthesized compounds displayed moderate to satisfactory AR binding affinity and might lead to antagonist activity against AR. Among them, compound A16 exhibited the best AR binding affinity (85%) and degradation activity against AR. Due to the strong fluorescence properties of pomalidomide derivatives, B10 was found to be effectively internalized and visualized in LNCaP (AR + ) cells than PC-3 (AR-) cells. Moreover, the molecular docking of A16 with AR and the active site of DDB1-CRBN E3 ubiquitin ligase complex provides guidance to design new PROTAC degrons targeting AR for prostate cancer therapy. These results represent a step toward the development of novel and improved AR PROTACs.
Fluorescent probe targeting androgen receptor, and preparation method thereof
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Paragraph 0047; 0048, (2020/02/20)
The invention discloses a fluorescent probe targeting an androgen receptor, and a preparation method thereof, particularly relates to an AR fluorescent probe obtained by linking a pomalidomide fluorophore to an androgen receptor (AR) non-steroidal antagonist skeleton, and belongs to the field of medicinal chemistry. According to the invention, the fluorescent probe has a structural general formuladefined in the specification, and can selectively image androgen receptor high-expression cells at the cellular level, and the synthesis process is simple and feasible, cheap and easily available inraw materials, low in preparation cost and easy to popularize.
AZA-PHENALENE-3-KETONE DERIVATIVE, PREPARATION METHOD THEREOF, AND ITS APPLICATION AS PARP INHIBITOR
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Paragraph 0020, (2018/05/26)
Disclosed are an aza-phenalene-3-ketone derivative, a preparation method thereof and its application as a PARP inhibitor. The aza-phenalene-3-ketone derivative has the following structure: wherein R is hydrogen, methyl, ethyl, isopropyl, benzyl or 3-methyl-3-butenyl. The aza-phenalene-3-ketone derivative has very high activity for inhibiting PARP, thereby providing a good basis for new drug research of developing a nitrogen-doped phenalene-3-ketone compound as PARP inhibitor to treat cancer.
