Marine natural products: highly functionalized steroids (12β-hydroxy-24-norcholesta-1,4,22-trien-3-one and 12β-acetoxy-24-norcholesta-1,4,22-trien-3-one) from the sea raspberry, Gersemiarubiformis
Treatment of 2-(2-formyl-1H-pyrrol-1-yl)-3-thiophenecarbonitrile by sodium percarbonate afforded, in a one-pot sequence and on a multigram scale, 5,6-dihydro-6-hydroxy-4H-pyrrolo[1,2-a]thieno-[3,2-f][1,4]diazepin-4-one whose reactivity towards various nucleophiles like amines, hydrazines and thiols was evaluated.
用一锅顺序并以克数计提供的过碳酸钠处理过碳酸氢钠处理2-(2-甲酰基-1 H-吡咯-1-基)-3-噻吩甲腈5,6-二氢-6-羟基-4 H-吡咯并[1,2- a ]噻吩并-[3,2- f ] [1,4]二氮杂-4--1-酮被评估了其对各种亲核试剂如胺,肼和硫醇的反应性。
Fe<sub>2</sub>(SO<sub>4</sub>)<sub>3</sub>·xH<sub>2</sub>O on silica: an efficient and low-cost catalyst for the direct nucleophilic substitution of alcohols in solvent-free conditions
Fe2(SO4)3·xH2O on silica has been found to be a novel efficient catalyst for the direct nucleophilic substitution of alcohols in solvent-free conditions. In this reaction system, the alcohols can react with various nucleophilic reagents for the convenient construction of C–C bonds and C–N bonds with the benefits of high conversion, no requirement to use excessive amounts of the nucleophile, only a catalytic amount of iron catalyst required, solvent-free and benign reaction conditions, and the feasible reusability of the catalyst.
New pyrazolopyridine analogs: Synthesis, antimicrobial, antiquorum-sensing and antitumor screening
作者:N.S. El-Gohary、M.I. Shaaban
DOI:10.1016/j.ejmech.2018.04.025
日期:2018.5
MCF-7 cells. The most active in vitro antitumoranalogs, 2, 4, 5 and 7 were assessed for in vivo antitumor efficacy on Ehrlich ascites carcinoma (EAC) cells, whereas compound 5 displayed the highest efficacy. In addition, cytotoxicity testing toward W138 and WISH normal cells revealed that all tested analogs are less cytotoxic than doxorubicin. The new analogs were evaluated for DNA-binding affinity, whereas
Nouveaux dérivés de la 4H-pyrrolo[1,2-a]thieno[3,2-f][1,4]-diazépine leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
申请人:ADIR ET COMPAGNIE
公开号:EP0446133A1
公开(公告)日:1991-09-11
L'invention concerne des composés de formule générale I :
dans laquelle :
- R1 représente un radical de formule générale (Z0), (Z1), (Z2), (Z3) ou (Z4)
- R2 représente un radical methylène, un radical hydroxymethylène, un radical carbonyle, un radical de formule générale (Y1), (Y2), (Y3) ou (Y4) :
ou forme avec R12 et l'atome d'azote auxquels ils sont rattachés un radical de formule générale (W) :
R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 et n étant tels que définis dans la description. Médicaments.