Shanghai Blueray Biophanna focuses on First-in Class drug discovery of WD40 repeat（WDR）*** domain is one of the largest protein families from yeast to human,consisting about 1%total cell *** proteins generally funct...
详细信息
Shanghai Blueray Biophanna focuses on First-in Class drug discovery of WD40 repeat（WDR）*** domain is one of the largest protein families from yeast to human,consisting about 1%total cell *** proteins generally function as platform of protein-protein interactions and are involved in a wide range of cellular ***,a subunit of PRC2 complex,is an important member of WDR family and plays critical role of methylating H3 ***,a novel class of EED inhibitors,represented by BRSS4 with great drug-like properties,in vivo efficacy and favorable toxicology profile,will be presented.
MB06322(CS-917,a prodrug of FBPase inhibitor MB05032) significantly lowered fasting plasma glucose levels in patients with type 2 diabetes(T2DM) during two phase 2a clinical *** 2nd-generation program sought to improv...
详细信息
MB06322(CS-917,a prodrug of FBPase inhibitor MB05032) significantly lowered fasting plasma glucose levels in patients with type 2 diabetes(T2DM) during two phase 2a clinical *** 2nd-generation program sought to improve a number of properties of MB06322including oral bioavailability and efficient conversion of the prodrug to the active phosphonic
The Formal synthesis of an antitumor antibiotic,fostriecin,via a highly convergent route is described.A characteristic feature of the present synthesis is that the synthesis was achieved via a coupling procedure of th...
详细信息
The Formal synthesis of an antitumor antibiotic,fostriecin,via a highly convergent route is described.A characteristic feature of the present synthesis is that the synthesis was achieved via a coupling procedure of three segments A,B,and *** segment A,a α,β,-unsaturated 8-lactone was constructed via a coupling,iodolactonization and dehydration *** segment B,with chiral tertiary and secondary alcohols,was prepared via[2,3]-Meisenheimer rearrangement,epoxidation and epoxy-ring *** two segments were coupled using the Julia-Kocienski olefination.
The Spingosine-1-phosphate receptor 1(S1P1) has been proven to be a potential target for autoimmune ***720 the represented 2-aminopropane-1,3-diol agent has been approved for the treatment of relapsing remitting multi...
详细信息
The Spingosine-1-phosphate receptor 1(S1P1) has been proven to be a potential target for autoimmune ***720 the represented 2-aminopropane-1,3-diol agent has been approved for the treatment of relapsing remitting multiple sclerosis(MS).The clinical efficacy of FTY720 and the understanding of what cause its side effects have initiate intensive efforts toward the discovery of
A novel and efficient method for the one-pot synthesis of 2 H-indazole from readily available building blocks is *** reaction of 2-nitrobenzylamines with zinc and ammonium formate underwent partial reduction to nitros...
详细信息
A novel and efficient method for the one-pot synthesis of 2 H-indazole from readily available building blocks is *** reaction of 2-nitrobenzylamines with zinc and ammonium formate underwent partial reduction to nitroso benzylamine followed by an intramolecular cyclization to afford 2 H-indazole via N-N bond *** carboxylic acid moiety of indazole was proceeded to regioselective alkyne insertion under ruthenium catalysis to form pyranone-fused *** regioselectivity is influenced by the weak co-ordination of indazole ring nitrogen to the metal center.
It is reported that transmembrane anion/cation symport can induce cell death by disrupting the ionic homeostasis of cells. Herein,we designed and synthesized aza-crown ether-squaramide conjugates and studied their ani...
详细信息
It is reported that transmembrane anion/cation symport can induce cell death by disrupting the ionic homeostasis of cells. Herein,we designed and synthesized aza-crown ether-squaramide conjugates and studied their anion/cation symport properties and anti-tumor activity（Fig.1）.The results indicate that these conjugates exhibit potent liposomal and in vitro anion/cation symport,and are able to trigger cell apoptosis by modifying the intracellular pH,inducing the basification of acidic organelles in live cells and facilitating the influx of chloride and sodium ions into cells.
Ferrocenyl Schiff bases were synthesized with ferrocenecarboxaldehyde and reducted to secondary amines as *** earth complexes synthesized with these ligands have been characterized by ESI-MS,single-crystal X-ray dif&a...
详细信息
Ferrocenyl Schiff bases were synthesized with ferrocenecarboxaldehyde and reducted to secondary amines as *** earth complexes synthesized with these ligands have been characterized by ESI-MS,single-crystal X-ray dif&action *** cellular level,antitumor activity of the ligands and its complexes has been examined by MTT assay and flow *** molecular level,the interaction of complexes with DNA were investigated by UV-vis,fluorescence,CD spectroscopy,viscosity and agraose gel electrophoresis.
Steroids heterocyclic compounds formed by the fusion of A rings or D rings with heterocycles usually have good biological activities,and they have received extensive attention from pharmaceutical *** dehydroepiandrost...
详细信息
Steroids heterocyclic compounds formed by the fusion of A rings or D rings with heterocycles usually have good biological activities,and they have received extensive attention from pharmaceutical *** dehydroepiandrosterone as the staring material,we have synthesized a series of 15β,16β-methylene steroid-2-benzylidene-4,6-diene-3,17-dione *** reaction process is shown in Scheme *** the final structures are first reported and identified by NMR spectroscopys,and the yields of these products are moderate to good and the reaction conditions are *** in vitro cytotoxicity of this novel derivatives are undergoing.
A photochemical avenue to synthesize nitrogen-rich quantum dots（N-dots） using 2-azido imidazole as the starting material was established for the first time[1,2].A production yield of up to 92.7%was *** N-dots were t...
详细信息
A photochemical avenue to synthesize nitrogen-rich quantum dots（N-dots） using 2-azido imidazole as the starting material was established for the first time[1,2].A production yield of up to 92.7%was *** N-dots were then fully characterized by elemental analysis,IR,XPS,XRD,AFM and *** the basis of the N production and in situ IR results,the underlying mechanism for the photochemical formation of N-dots was *** N-dots showed promising optical properties including wavelength-dependent upconversion photoluminescence,and were successfully used in upconversion cell imaging[3].
Brefeldin A is a macrolide antibiotic synthesized by fungi that inhibits protein transportation from the endoplasmic reticulum to the Golgi apparatus by blocking the formation of COPII envelope *** A displays anti-fun...
详细信息
Brefeldin A is a macrolide antibiotic synthesized by fungi that inhibits protein transportation from the endoplasmic reticulum to the Golgi apparatus by blocking the formation of COPII envelope *** A displays anti-fungal,anti-viral and anti-mitotic *** is also widely used in bio-signaling *** to unique location,novel structure and non-interaction with other traditional insecticides,the inhibitors of uridin receptors have attracted researchers' *** to the principle of drug combination,we spliced the pharmacophore of the uridin receptor pesticide and the protein transport inhibitor brefeldin A to obtain a series of biomimic insecticides and studied the biological activity,structure-activity relationship and the target of action.
暂无评论