2201-24-3Relevant articles and documents
Spiro [benzo [c] aza-1, 1 '-cyclohexyl]-3-ketone compound
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Paragraph 0050; 0055-0056, (2021/06/12)
The invention belongs to the technical field of medicines, relates to a compound with anti-tumor activity and a specific chemical structure, and particularly relates to a 4, 5-dihydrospiro [benzo [c] aza-1, 1 '-cyclohexyl]-3 (2H)-ketone compound as well as a preparation method and application of the 4, 5-dihydrospiro [benzo [c] aza-1, 1'-cyclohexyl]-3 (2H)-ketone compound. The structural general formula of the compound is shown in the specification, wherein an R group on an a benzene ring is substituted by a 2-position, 3-position or 4-position monosubstituted fluorine atom, methyl, chlorine atom, methoxyl, bromine atom or hydrogen atom. Pharmacological studies show that the compound provided by the invention has certain inhibitory activity on human colon cancer HCT-116 cells, can be used for preparing antitumor drugs, and opens up a new way for deep research and development of tumor drugs in the future. The preparation method provided by the invention is simple and feasible, relatively high in yield and easy for large-scale production.
1-azaspiro[5.5]undecyl-3-one and 1-azaspiro[5.5]undecyl-3-alcohol compounds
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Paragraph 0078; 0083-0084, (2020/05/30)
The invention belongs to the technical field of medicines, and particularly relates to 1-azaspiro[5.5]undecyl-3-one and 1-azaspiro[5.5]undecyl-3-alcohol compounds and a preparation method and application thereof. The general formulas of the 1-azaspiro[5.5]undecyl-3-one compound and the 1-azaspiro[5.5]undecyl-3-alcohol compounds are shown in a formula I and a formula II in the specification. A six-membered spiro structure is synthesized for the first time, a brand-new compound with a better anti-tumor effect is obtained, and pharmacological research shows that the compound has certain inhibitory activity on human colon cancer HCT-116 cells. The preparation method of the 1-azaspiro[5.5]undecyl-3-one compound and the 1-azaspiro[5.5]undecyl-3-alcohol compound is simple and feasible, the yieldis relatively good, and the method is suitable for industrial production.
Design, synthesis and biological evaluation of homoerythrina alkaloid derivatives bearing a triazole moiety as PARP-1 inhibitors and as potential antitumor drugs
Li, Shuai,Li, Xin-yang,Zhang, Ting-jian,Kamara, Mohamed Olounfeh,Liang, Jing-wei,Zhu, Ju,Meng, Fan-hao
, (2019/11/11)
A series of homoerythrina alkaloid derivatives containing a 1,2,3-triazole moiety as PARP-1 inhibitors were designed and synthesized. And their anti-proliferative activity was further evaluated. Compound 10n had excellent activity to inhibit proliferation of A549 cells (IC50 = 1.89 μM), which was higher than harringtonine (IC50 = 10.55 μM), pemetrexed (IC50 = 3.39 μM), and rucaparib (IC50 = 4.91 μM). Furthermore, the selectivity index of compound 10n was higher than rucaparib and pemetrexed for lung cancer cells. Flow cytometry analysis showed that compound 10n significantly arrested the cell cycle in the S phase, then induced apoptosis of A549 cells (apoptosis rate is 46%), which effectively inhibited cell proliferation. Simultaneously, western blot analysis revealed that compound 10n could prevent the biosynthesis of PAR. Further analysis results revealed that compound 10n could inhibit the expression of cyclin A, down-regulate the expression of bcl-2/bax, activate caspase-3, and ultimately induce apoptosis of A549 cells. All the results indicated that compound 10n had potential research value as a novel PARP-1 inhibitor in antitumor, and it provided a new reference for further development of PARP-1 inhibitors.