- Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer
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Prostate cancer (PC) is the most common malignancy in men worldwide. Here, two series of novel thiohydantoin derivatives of enzalutamide as potent androgen receptor (AR) antagonists were designed and synthesized. Among them, compound 31c was identified as an AR antagonist which is 2.3–fold more potent than enzalutamide. Molecular docking studies were performed to explain the improved potency of 31c at AR. In cell proliferation assays, 31c exhibited similar anti-proliferative activities with enzalutamide against hormone sensitive LNCaP cells and AR-overexpressing LNCaP/AR cells. These data indicate that 31c can be a good lead compound for further structure optimization for the treatment of prostate cancer.
- Wang, Ao,Wang, Yawan,Meng, Xin,Yang, Yushe
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- Enantioselective Synthesis of 2-Functionalized Tetrahydroquinolines through Biomimetic Reduction
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Biomimetic asymmetric reduction of 2-functionalized quinolines has been successfully developed with the chiral and regenerable NAD(P)H model CYNAM in the presence of transfer catalyst simple achiral phosphoric acids, providing the chiral 2-functionalized
- Zhao, Zi-Biao,Wang, Jie,Zhu, Zhou-Hao,Chen, Mu-Wang,Zhou, Yong-Gui
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supporting information
p. 9112 - 9117
(2021/11/24)
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- B(C6F5)3-catalyzed metal-free hydrogenations of 2-quinolinecarboxylates
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A metal-free hydrogenation of 2-quinolinecarboxylates has been realized by using 5 mol% of B(C6F5)3 as catalyst. A variety of tetrahydroquinolines were obtained in 57–99% yields. An attempt for the asymmetric hydrogenation with chiral boron Lewis acids generated from chiral dienes afforded very low ee's.
- Han, Caifang,Zhang,Feng, Xiangqing,Wang, Shoufeng,Du, Haifeng
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supporting information
p. 1400 - 1403
(2018/03/12)
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- Thio hydantoin ternary and circular androgen receptor antagonists and use thereof (by machine translation)
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The invention relates to the field of pharmaceutical chemistry, and in particular relates to a category of thio hydantoin and indoline skeleton has the role of the anti-prostate cancer compound (I) and (II), a method for preparing these compounds, these c
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Paragraph 0193; 0208; 0209
(2017/08/02)
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- ACYLATED INDOLINE AND TETRAHYDROQUINOLINE DERIVATIVES AS HCV INHIBITORS
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Use of a compound of Formula (I) : wherein: R1 represents hydroxy or NR BRC; R2 represents C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; R3 represents aryl or heteroaryl; Rsu
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Page/Page column 58
(2010/02/09)
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- Novel N-acylated heterocycles
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Described are compositions comprising a muscarinic receptor antagonist and an N-acylated heterocycle derivative having affinity for serotonergic receptors, and enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts thereof. The combination of a muscarinic receptor antagonist and an N-acylated heterocycle, or an enantiomer, diastereoisomer, N-oxide, polymorph, solvate or pharmaceutically acceptable salt thereof, is useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptors.
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