- Design, synthesis, and cytotoxic activity of novel 2H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidine derivatives
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In this study, a series of novel 2H-imidazo [1, 2-c] pyrazolo [3, 4-e] pyrimidine derivatives were designed, synthesized, and evaluated for their cytotoxic activities. The in vitro cell growth inhibition assay of the target compounds indicated their selectivity in inhibiting the proliferation of blood tumor cells (K562, U937) and solid tumor cells (HCT116, HT-29). Compound 9b exhibited the highest antiproliferative activities against K562 (IC50 = 5.597 μM) and U937 (IC50 = 3.512 μM). Based on the flow cytometry assays, compound 9b caused obvious induction of cell apoptosis and cell arrest at the S phase. Furthermore, western blot analysis revealed that compound 9b upregulated the expression of Bax, downregulated the levels of Bcl-2, and further activated caspase-3 in K562 cells. Therefore, compound 9b may be a potential anticancer agent that deserves further investigation.
- Zheng, You-Guang,Pei, Xin,Xia, De-Xin,Wang, Yuan-Bo,Jiang, Ping,An, Lin,Huang, Tong-Hui,Xue, Yun-Sheng
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- Pyrazole-pyrimido imidazole compound as well as preparation method and application thereof
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The invention relates to a pyrazole-pyrimido imidazole compound as well as a preparation method and application thereof, and belongs to the field of medicinal chemistry and pharmacotherapeutics. The invention provides application of the compound shown in the formula I or the pharmaceutically acceptable salt thereof in preparation of drugs for treating tumor-related diseases.
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Paragraph 0067-0069
(2020/04/22)
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- 3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00355; 00356; 00357
(2017/09/27)
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- PH fluorescent probe by taking pyridine as protonizing site and application thereof
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The invention relates to the technical field of detection, and particularly relates to a novel compound by using 4-(5-phenyl-2-oxazolyl)pyridine as a kernel structure as shown in the general formula (I), as well as a chemical preparation process of the pH fluorescent probe. According to the compound, R1, R2 and R3 are halogen atoms, nitrogen atoms, alkyl, alkoxy or group as shown in the formula IA, wherein Y is a group formed by covalent linkage of methylene, oxygen atom or nitrogen atom with a group as shown in a formula IB (in the formula IB, R5 is hydrogen atom, alkyl or alkoxy, Z1, Z2 and Z3 are null or oxygen atoms, and n, o and p are 0, 1 or 2; R4 represents hydrogen atom, methyl, methoxyl or a group as shown in the formula IB, and m is 0, 1 or 2; R1, R2 and R3 are not halogen atom, hydrogen atom, alkyl or alkoxy at the same time, and X is CH=CH or null, namely a biphenyl structure. The chemical preparation process is applied to fluorescent probe detection on pH value in an aqueous solution, fluorescent probe detection on the pH value in a cell, especially fluorenscense angiography of cells.
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Paragraph 0056; 0060
(2017/08/31)
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- The reductive cleavage of picolinic amides
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Treatment of picolinic amides with excess zinc in aqueous hydrochloric acid at room temperature affords the corresponding amines in good to excellent yields. The mild reaction conditions exhibit useful functional group tolerance and facilitate the application of the picolinic amide moiety as a protecting group which can be easily introduced and selectively removed.
- O'Donovan, Daniel H.,De Fusco, Claudia,Spring, David R.
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supporting information
p. 2962 - 2964
(2016/07/06)
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- Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists
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A new series of morpholine derivatives has been identified as selective DA D3 receptor antagonists; their in vitro profile and pharmacokinetic data are provided.
- Micheli, Fabrizio,Cremonesi, Susanna,Semeraro, Teresa,Tarsi, Luca,Tomelleri, Silvia,Cavanni, Paolo,Oliosi, Beatrice,Perdon, Elisabetta,Sava, Anna,Zonzini, Laura,Feriani, Aldo,Braggio, Simone,Heidbreder, Christian
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p. 1329 - 1332
(2016/02/23)
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- Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: From lead to clinical compound
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Rapid clinical progress of hepatitis C virus (HCV) replication inhibitors, including these selecting for resistance in the NS5A region (NS5A inhibitors), promises to revolutionize HCV treatment. Herein, we describe our explorations of diverse spiropyrrolidine motifs in novel NS5A inhibitors and a proposed interaction model. We discovered that the 1,4-dioxa-7-azaspiro[4.4]nonane motif in inhibitor 41H (GSK2236805) supported high potency against genotypes 1a and 1b as well as in genotype 1b L31V and Y93H mutants. Consistent with this, 41H potently suppressed HCV RNA in the 20-day RNA reduction assay. Pharmacokinetic and safety data supported further progression of 41H to the clinic.
- Kazmierski, Wieslaw M.,Maynard, Andrew,Duan, Maosheng,Baskaran, Sam,Botyanszki, Janos,Crosby, Renae,Dickerson, Scott,Tallant, Matthew,Grimes, Rick,Hamatake, Robert,Leivers, Martin,Roberts, Christopher D.,Walker, Jill
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p. 2058 - 2073
(2014/04/03)
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- 5-(4-Bromophenyl)oxazole
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The compound 5-(4-bromophenyl)oxazole is useful as an antifungal agent.
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- 1-[[[5-(Substituted phenyl)-2-oxazolyl]methylene]amino]-2,4-imidazolidinediones
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A series of 1-[[[5-(substituted phenyl-2-oxazolyl]methylene]amino]-2,4-imidazolidinediones are useful as muscle relaxants.
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