Search results for "Azocine"
showing 10 items of 28 documents
Eight-membered heterocycles with two heteroatoms in a 1,2-relationship of interest in medicinal chemistry
2021
Abstract This chapter treats 1,2-diheterocines, eight membered heterocyclic systems with two heteroatoms, N, O and S, in an 1,2 relationship, exhibiting biological properties and exhaustively covers the literature from 2007 to the end of November 2019. In this period of time 1,2-diazocine, 1,2-oxazocine, 1,2-dioxocin and 1,5-dithiocin ring systems had derivatives exhibiting pharmacological activities. No articles on biological properties have been reported for 1,2-thiazocines and 1,2-oxathiocins. Besides uncondensed derivatives, 1,2-diheterocines fused with five-, six-, and seven-membered carbocycles or heterocycles have been reviewed, as well as bridged 1,2-diheterocines.
Eight-Membered Rings With Two Heteroatoms 1,5
2022
This chapter titled “Eight-membered Rings with two Heteroatoms 1,5” deals eight-membered rings with two heteroatoms in a 1,5-relationship, namely 1,5-diazocine, 1,5-oxazocine, 1,5-thiazocine, 1,5-dioxocin, 1,5-oxathiocin, and 1,5-dithiocin and covers the literature from 2007 to October 2020 (SciFindern search) reporting the chemistry of uncondensed derivatives, diheterocines fused to carbocycles and heterocycles, as well as bridged diheterocines. Among them, the 1,5-diazocine ring system is by far the largest class, based on the number of publications which constituted the 87% of the total amount of the references reported in the range of interest of CHEC IV. Thus, 1,5-diazocines were divid…
Synthesis and antiproliferative activity of new derivatives containing the polycyclic system 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3’,4’:2,3]azep…
2013
The reaction under reflux between 1-phenyl-3-R-5-methylaminopyrazoles and 2,5-hexanedione lead to 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3′,4′:2,3]azepino[4,5-f]azocine derivatives 3b–g. These unusual molecules show the structural complexity of many biologically active natural products and are endowed with the chemical diversity that is required in drug discovery. The compounds 3b,e were reduced by hydrogen in the presence of Palladium on activated charcoal to give the dihydro derivatives 5b,e. Compounds 3b–f and 5b,e were selected by the NCI to evaluate their in vitro antiproliferative activity against 60 human cell lines derived from nine clinically isolated cancer types (leukaemia, lu…
Synthesis and antioproliferative activity of new derivatives containing the policyclic sistem 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3'.4':2,3]aze…
2012
By reacting methylaminopyrazoles with hexane-2,5-dione in 1,4-dioxane in the presence of p-toluensulfonic acid, new derivatives containing the policyclic sistem 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3'.4':2,3]azepino[4,5-f]azocine were obtained. The new synthesized compounds were tested preliminarly at 10 microM against five human cancer cell lines showing a range of inhibition of 20-62% against the most susceptible cell lines K562 and HCT116.
CCDC 655687: Experimental Crystal Structure Determination
2008
Related Article: H.V.Ly, H.M.Tuononen, M.Parvez, R.Roesler|2008|Angew.Chem.,Int.Ed.|47|361|doi:10.1002/anie.200703556
CCDC 1546697: Experimental Crystal Structure Determination
2017
Related Article: Adam F. Henwood, Amlan K. Pal, David B. Cordes, Alexandra M. Z. Slawin, Thomas W. Rees, Cristina Momblona, Azin Babaei, Antonio Pertegás, Enrique Ortí, Henk J. Bolink, Etienne Baranoff, Eli Zysman-Colman|2017|J.Mater.Chem.C|5|9638|doi:10.1039/C7TC03110F
CCDC 1979408: Experimental Crystal Structure Determination
2021
Related Article: Widukind Moormann, Tobias Tellkamp, Eduard Stadler, Fynn R��hricht, Christian N��ther, Rakesh Puttreddy, Kari Rissanen, Georg Gescheidt, Rainer Herges |2020|Angew.Chem.,Int.Ed.|59|15081|doi:10.1002/anie.202005361
CCDC 1546698: Experimental Crystal Structure Determination
2017
Related Article: Adam F. Henwood, Amlan K. Pal, David B. Cordes, Alexandra M. Z. Slawin, Thomas W. Rees, Cristina Momblona, Azin Babaei, Antonio Pertegás, Enrique Ortí, Henk J. Bolink, Etienne Baranoff, Eli Zysman-Colman|2017|J.Mater.Chem.C|5|9638|doi:10.1039/C7TC03110F
New complex polycyclic compounds: Synthesis, antiproliferative activity and mechanism of action
2020
Abstract Polycyclic or O-glycoconiugate polycyclic compounds 1a-g were previously tested for their in vitro antiproliferative activity. In this series of compounds, activity increases as log P decreases. Specifically, compounds 1d and 1g showed lower log P values together with the best antiproliferative profiles. With the aim of extending our understanding of the structure–activity relationship (SAR) of this class of compounds, we prepared new polycyclic derivatives 2a-c, which bear on each of the two phenyl rings hydrophilic substituents (OH, SO2NH2 or NHCOCH3). These substituents are able to form hydrogen bonds and to decrease the partition coefficient value as compared with compound 1d. …
(E)-2-{[1-(3,11-Dimethyl-4-methylene-10-oxo-1-phenyl-4,5,10,11-tetrahydro-1H-benzo[b]pyrazolo[3,4-f][1,5]diazocin-5-yl)ethylidene]amino}-N-methyl-N-(…
2013
The central eight-membered ring of the title compound, C40H36N8O2, deviates from the ideal boat conformation because the bond between the exo-ethylene group and the adjacent N atom is twisted by 60.0 (4)° due to steric hindrance. Its adjacent benzene and pyrazole rings are oriented almost perpendicular to each other, making a dihedral angle of 85.8 (3)°. In the crystal, the molecules are linked by C(ar)—H...O hydrogen bonds, generating a three-dimensional network.