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Raoling Ge
China Pharmaceutical University
8Publications
4H-index
36Citations
Publications 8
Newest
#1Pengfei Xu (CPU: China Pharmaceutical University)H-Index: 2
#2Hongyu Luan (CPU: China Pharmaceutical University)H-Index: 1
Last.Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
view all 11 authors...
Ulipristal acetate (UPA) was developed by Laboratoire HRA Pharma, France and approved by the FDA for emergency contraception in August 2010. Though several methods have been developed for the synthesis of UPA, the steroidal impurities would appear inevitably and have not been reported in detail. In this work, several stereoisomeric and N,N-didemethylated impurities of UPA were analyzed and synthesized. The stereoisomers were obtained through an efficient and practical approach, and the structure...
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#1Raoling Ge (CPU: China Pharmaceutical University)H-Index: 4
#2Xi Xu (CPU: China Pharmaceutical University)H-Index: 5
Last.Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
view all 6 authors...
Prostate cancer is the most common carcinoma among aged males in western countries and more aggressive and lethal castration resistant prostate cancer often occurs after androgen deprivation therapy. The high expression of androgens and androgen receptor is closely related to prostate cancer. Efficient androgen receptor antagonists, such as enzalutamide and ARN-509, could be employed as potent anti-prostate cancer agents. Nevertheless, recent studies have revealed that F876L mutation in androgen...
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#1Xi Xu (CPU: China Pharmaceutical University)H-Index: 5
#2Raoling Ge (CPU: China Pharmaceutical University)H-Index: 4
Last.Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
view all 9 authors...
Abstract Prostate cancer (PC) is a major cause of cancer-related male death in worldwide and the identification of new and improved potent anti-PC molecules is constantly required. A novel scaffold of tetrahydroisoquinoline thiohydantoin was rationally designed based on the enzalutamide structures and our pre-work, leading to the discovery of a series of new antiproliferative compounds. Several new analogues displayed improved androgen receptor (AR) antagonistic activity, while maintaining the h...
5 CitationsSource
#1Pengfei Xu (CPU: China Pharmaceutical University)H-Index: 2
#2Xi Feng (CPU: China Pharmaceutical University)H-Index: 1
Last.Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
view all 7 authors...
Abstract P2Y receptors are G-protein-coupled receptors (GPCRs) for extracellular nucleotides. There are eight mammalian P2Y receptor subtypes (P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, and P2Y14). P2Y2 receptors are widely expressed and play important roles in multiple functionalities. Diquafosol tetrasodium, known as INS365, which was the first P2Y2 receptor agonists that had been approved in April 2010 and launched in Japan by Santen Pharmaceuticals. Besides, a series of similar agonists fo...
1 CitationsSource
#1Jubo Wang (CPU: China Pharmaceutical University)H-Index: 1
#2Raoling Ge (CPU: China Pharmaceutical University)H-Index: 4
Last.Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
view all 7 authors...
Abstract Phenotypic screening of high quality compound library is one of the most effective strategy to obtain novel bioactive compounds. Recently, our group have constructed a Wogonin-scaffold library with substituents diversity and successfully obtained a series of potent compounds. Herein, we reported the synthesis of these compounds and evaluated the in vitro antitumor activity against a panel of human tumor cell lines. Most of them showed good activity with a broad spectrum and preliminary ...
3 CitationsSource
#1Minzan Zuo (CPU: China Pharmaceutical University)H-Index: 1
#2Xi Xu (CPU: China Pharmaceutical University)H-Index: 5
Last.Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
view all 7 authors...
Abstract A novel scaffold of indoline thiohydantoin was discovered as potent androgen receptor (AR) antagonist through rational drug designation. Several compounds showed good biological profiles in AR binding and higher selective toxicity than enzalutamide toward LNCaP cells (AR-rich) versus DU145 cells (AR-deficient). In addition, the docking studies supported the rationalization of the biological evaluation. Among these compounds, the representative compound 48c exhibited the strongest inhibi...
14 CitationsSource
#1Raoling Ge (CPU: China Pharmaceutical University)H-Index: 4
#2Qian Zhao (CPU: China Pharmaceutical University)H-Index: 4
Last.Li Zhao (CPU: China Pharmaceutical University)H-Index: 30
view all 7 authors...
Abstract The design and synthesis of a new series of 6-fluoro-3-phenyl-7-piperazinyl quinolone derivatives, built on the structure of 1-ethyl-3-(6-nitrobenzoxazol-2-yl)-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4(1H)-quinolone, are described. These compounds provide new scaffold for the discovery of Topoisomerase I (Top I) inhibitors and target based assay showed that they can obviously inhibited Top I at 100 μM. The in vitro anti-proliferative activity of these new compounds was evaluated against...
7 CitationsSource
#1Minzan ZuoH-Index: 2
#2Xi XuH-Index: 5
Last.Zhiyu LiH-Index: 22
view all 5 authors...
Although prostate cancer can initially respond to androgen deprivation therapy, it will inevitably relapse and switch to a castration-resistant state. The progress in understanding the mechanism of castration-resistant prostate cancer (CRPC) has led to the evolution of novel agents, including sipuleucel-T as an immunomodulant agent, enzalutamide as an androgen receptor antagonist, docetaxel as a chemotherapeutic agent and radium-223 as a radiopharmaceutical agent. In this review, we discuss the ...
6 CitationsSource
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