- FUSED RING PYRIMIDINE COMPOUND, INTERMEDIATE, AND PREPARATION METHOD, COMPOSITION AND USE THEREOF
-
Disclosed area fused ring pyrimidine compound, and an intermediate, a preparation method, a composition and a use thereof. The fused ring pyrimidine compound is a compound as shown in formula I, a tautomer, an enantiomer, a diastereoisomer, a pharmaceutically acceptable salt, a metabolite, a metabolic precursor or a prodrug thereof, wherein the above-mentioned compound is used for the preparation of a medicine for preventing, remitting or treating one or more of immune system diseases, autoimmune diseases, cell proliferative diseases, allergic disorders and cardiovascular diseases, and the compound has a strong inhibitory effect on the Janues kinase, FGFR kinase, FLT3 kinase and Src family kinase.
- -
-
Paragraph 0204-0205
(2018/08/12)
-
- Synthesis of riccardin D derivatives as potent antimicrobial agents
-
We describe the synthesis and biological evaluation of riccardin D derivatives, a novel class of antimicrobial molecules. Structural diversification of these derivatives was achieved by introducing hydroxy, methoxy, and bromine into the aromatic rings of riccardin D. The antimicrobial evaluation of these compounds was performed as in vitro assays against clinically isolated bacteria and fungi. The introduction of bromine atom into the arene B of riccardin D led to several strongly active antibacterial compounds with a MIC value ranging from 0.5 to 4 μg/mL for Staphylococcus aureus, both methicillin-sensitive and -resistant strains. Antifungal tests found compound 34 was the most potent molecule with a MIC value of 2 μg/mL against Candida albicans. This initial biological evaluation suggests that these novel molecules merit further investigation as potential antimicrobial agents.
- Sun, Bin,Zhang, Ming,Li, Ying,Hu, Qing-wen,Zheng, Hong-bo,Chang, Wen-qiang,Lou, Hong-Xiang,Lou, Hong-xiang
-
supporting information
p. 3617 - 3620
(2016/07/21)
-
- Synthesis of macrocyclic bisbibenzyl derivatives and their anticancer effects as anti-tubulin agents
-
Based on the core skeleton of the total synthesized bisbibenzyl marchantin C, riccardin D and plagiochin E, a series of brominated and aminomethylated derivatives of above three bisbibenzyls have been synthesized and their cytotoxic activity against KB, M
- Jiang, Juan,Sun, Bin,Wang, Yan-Yan,Cui, Min,Zhang, Li,Cui, Chang-Zhi,Wang, Yan-Feng,Liu, Xi-Gong,Lou, Hong-Xiang
-
p. 2382 - 2391
(2012/05/05)
-
- Ring strain and total syntheses of modified macrocycles of the isoplagiochin type
-
Macrocycles of the bisbibenzyl-type are natural products that are found exclusively in bryophytes (liverworts). The molecular framework of the subtype "isoplagiochin" is of substantial structural interest because of the chirality of the entire molecule, w
- Speicher, Andreas,Backes, Timo,Hesidens, Kerstin,Kolz, Juergen
-
supporting information; experimental part
(2010/04/22)
-
- A synthesis-driven structure revision of 'plagiochin E', a highly bioactive bisbibenzyl
-
Recently, a bisbibenzyl named plagiochin E showing remarkable antifungal and antitumor activities was isolated from Marchantia polymorpha, a liverwort. The total synthesis of the proposed structure for plagiochin E and of two structurally and biosynthetic
- Speicher, Andreas,Groh, Matthias,Zapp, Josef,Schauml?ffel, Anu,Knauer, Michael,Bringmann, Gerhard
-
scheme or table
p. 1852 - 1858
(2009/12/05)
-
- Syntheses of macrocyclic bisbibenzyls on solid support
-
We describe a route for the polymer supported total synthesis of the cyclic bisbibenzyls of the isoplagiochin type found in liverworts. TentaGel resins were used as solid support for a sequence involving Suzuki, Wittig and hydrogenation protocols. The pol
- Speicher, Andreas,Backes, Timo,Grosse, Stefan
-
p. 11692 - 11696
(2007/10/03)
-