Day: October 17, 2022

Mohammadi, Ali; Eshghi, Hossein; Bakavoli, Mehdi; Hadizadeh, Farzin; Moradi, Hassanali published the artcile< Synthesis of novel 3-substituted-5H-benzo[5,6][1, 4]thiazino[3,2-e][1,2,4]triazines and their 15-lipoxygenase inhibitory activity>, Synthetic Route of 4956-05-2, the main research area is benzothiazinotriazine preparation mol docking lipoxygenase inhibitor.

A new group of 3-substituted-5H-benzo[5,6][1,4]thiazino[3,2-e][1,2,4]triazines I (R = morpholin-4-yl, pyrrolidin-1-yl, 4-methylpiperidin-1-yl, etc.) was designed, synthesized and evaluated as inhibitors of 15-lipoxygenase (15-LO), and the results were compared with those of standard ligand 4-methyl-2-(4-methylpiperazin-1-yl)pyrimido[4,5-b][1,4]benzothiazine (4-MMPB). Among the newly designed ligands I, compound I (R = 4-phenylpiperazin-1-yl) showed the best IC50 of 15-LO inhibition (IC50 = 38 μM). The docking calculations were performed in MOE software based on the function of force-field scoring, in order to study the interaction of these new compounds I and standard ligand with 15-LO. The docking study implied that these ligands I have hydrogen bond interaction with the residue of active site of 15-LO.

Journal of the Iranian Chemical Society published new progress about Cyclic amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Synthetic Route of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Yoon, Hyung; Galls, Alexandra; Rozema, Soren D.; Miller, Scott J. published the artcile< Atroposelective Desymmetrization of Resorcinol-Bearing Quinazolinones via Cu-Catalyzed C-O Bond Formation>, Formula: C7H7ClN2O2, the main research area is resorcinol quinazolinone preparation enantioselective; quinazolinone aryl bromide Ullmann coupling atroposelective desymmetrization copper catalyst.

Enantioselective Cu-catalyzed C-O cross coupling reactions yielding atropisomeric resorcinol-bearing quinazolinones have been developed. By utilizing a new guanidinylated dimeric peptidic ligand, products I (R = H, Br, R1 = H, NO2, CF3, R2 = Me, Et, R3 = H, Me, OMe, R4 = H, OMe, X = CH; R = R1 = R3 = R4 = H, R2 = Me, X = N) were generated in good yields with excellent stereocontrol. The transformation was readily scalable and a range of product derivatizations were performed.

Organic Letters published new progress about Aryl bromides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Formula: C7H7ClN2O2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Chen, Yong; Wang, Xiaoyan; Xiang, Wei; He, Lin; Tang, Minghai; Wang, Fang; Wang, Taijin; Yang, Zhuang; Yi, Yuyao; Wang, Hairong; Niu, Ting; Zheng, Li; Lei, Lei; Li, Xiaobin; Song, Hang; Chen, Lijuan published the artcile< Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities>, HPLC of Formula: 89793-12-4, the main research area is purine hydroxamic acid derivative preparation histone deacetylase inhibitor cancer.

In the present study, a series of novel histone deacetylase (HDAC) inhibitors using the morpholinopurine as the capping group were designed and synthesized. Several compounds demonstrated significant HDAC inhibitory activities and antiproliferative effects against diverse human tumor cell lines. Among them, compound 10o was identified as a potent class I and class IIb HDAC inhibitor with good pharmaceutical profile and druglike properties. Western blot anal. further confirmed that 10o more effectively increased acetylated histone H3 than panobinostat (LBH-589) and vorinostat (SAHA) at the same concentration in vitro. In in vivo efficacy evaluations of HCT116, MV4-11, Ramos, and MM1S xenograft models, 10o showed higher efficacy than SAHA or LBH-589 without causing significant loss of body weight and toxicity. All the results indicated that 10o could be a suitable candidate for treatment of both solid and hematol. cancer.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, HPLC of Formula: 89793-12-4.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Lee, Kuan Han; Han, Chein Hwa; Hwang, Long Chih; Wang, Eng Chi; Tzeng, Cherng Chyi published the artcile< Acyclic nucleosides. Part 3: Synthesis of certain 1-[(1,3-dihydroxy-2-propoxy)methyl]-6-azauracils as potential antiviral agents>, Category: pyrimidines, the main research area is acyclic nucleoside azauracil preparation virucide; hydroxypropoxymethylazauracil acyclic nucleoside.

A number of 6-azauracils were trimethylsilylated and then coupled with 1,3-dibenzyloxy-2-chloromethoxypropane to give 1-[(1,3-dibenzyloxy-2-propoxy)methyl]-6-azauracils which were debenzylated with either BCl3 or Pd2O to yield the title compounds I (R = H, Me, Cl, Br).

Gaoxiong Yixue Kexue Zazhi published new progress about Acyclonucleosides Role: SPN (Synthetic Preparation), PREP (Preparation). 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia