83983-03-3Relevant articles and documents
Preparation method of olaparib impurity
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Paragraph 0010; 0016, (2021/01/30)
The invention discloses a preparation method of an olaparib impurity V. The compound V provided by the invention can be used as a reference substance for detecting olaparib related substances, and isused for purity control of olaparib bulk drugs and preparations. According to the preparation method, o-formylbenzoic acid is taken as an initial raw material, the compound V is obtained through condensation, substitution, dehydration and other operations, the method is high in selectivity, mild in condition and easy to operate, and the obtained product is high in purity.
Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists
Inoue, Kazumi,Urushibara, Ko,Kanai, Misae,Yura, Kei,Fujii, Shinya,Ishigami-Yuasa, Mari,Hashimoto, Yuichi,Mori, Shuichi,Kawachi, Emiko,Matsumura, Mio,Hirano, Tomoya,Kagechika, Hiroyuki,Tanatani, Aya
, p. 310 - 319 (2015/09/01)
The androgen receptor (AR) plays important roles in multiple physiological functions, including differentiation, growth, and maintenance of male reproductive organs, and also has effects on hair and skin. In this paper, we report the synthesis of nonsteroidal AR antagonists having a 4-benzyl-1-(2H)-phthalazinone skeleton. Among the synthesized compounds, 11c with two ortho-substituents on the phenyl group potently inhibited SC-3 cell proliferation (IC50: 0.18 μM) and showed high wt AR-binding affinity (IC50: 10.9 μM), comparable to that of hydroxyflutamide (3). Compound 11c also inhibited proliferation of LNCaP cells containing T877A-mutated AR. Docking study of 11c with the AR ligand-binding domain indicated that the benzyl group is important for the antagonism. These phthalazinone derivatives may be useful for investigating potential clinical applications of AR antagonists.