ChemInform Abstract: Acyl Derivatives of Cyclic Secondary Amines. Part 2. Dynamic 1H and 13C NMR Studies on Bis- and Tris-amides: Equilibria of syn-anti Interconversion

ChemInform ◽  
1988 ◽  
Vol 19 (14) ◽  
Author(s):  
A. R. KATRITZKY ◽  
R. MURUGAN ◽  
H. LUCE ◽  
B. C. CHEN ◽  
W. S. BREY ◽  
...  
1984 ◽  
Vol 83 (2) ◽  
pp. 79-85 ◽  
Author(s):  
Gian Carlo Stocco ◽  
Lorenzo Pellerito ◽  
Maria Assunta Girasolo ◽  
Alan G. Osborne

1994 ◽  
Vol 476 (1) ◽  
pp. 111-120 ◽  
Author(s):  
José L. García-Ruano ◽  
Isabel López-Solera ◽  
José R. Masaguer ◽  
M.A. Monge ◽  
Carmen Navarro-Ranninger ◽  
...  

2021 ◽  
Vol 33 (12) ◽  
pp. 3134-3138
Author(s):  
Rajnish K. Sharma ◽  
Malti Sharma ◽  
Yashpal Singh

2-Aminocyclopentene-1-carbodithioic acid (ACDA) and its N-/S-alkyl derivatives of methylsilicon(IV) chloride have been synthesized by the reactions of MeSiCl3 with sodium salt of ACDA and its N-/S-alkyl derivatives in 1:1 and 1:2 molar ratios. All these complexes have been characterized by elemental analysis, molecular weight measurements and spectroscopic (IR, 1H and 13C NMR) studies. The central silicon atom is coordinated to two sulphur atoms or one sulphur atom and one nitrogen atom of the ligand moiety in all of these derivatives, resulting in five and six coordination.


2019 ◽  
Vol 16 (5) ◽  
pp. 597-605 ◽  
Author(s):  
Evgenii Mozhaitsev ◽  
Evgenii Suslov ◽  
Yuliya Demidova ◽  
Dina Korchagina ◽  
Konstantin Volcho ◽  
...  

Background: Inhibition of the DNA repair enzyme, tyrosyl-DNA phosphodiesterase 1 (TDP1), may increase the efficacy of cancer drugs that cause damage to tumor cell DNA. Among the known TDP1 inhibitors, there are compounds containing moieties of natural substances, e.g., monoterpenoids. In this work, we synthesized several compounds containing aromatic/ heteroaromatic amines and monoterpenoid groups and assessed their TDP1 inhibition potential. Methods: Structures of all the synthesized compounds were confirmed by 1H and 13C NMR as well as HRMS. The TDP1 inhibitory activity of the amines was determined by real-time fluorescence oligonucleotide biosensor. Results: The synthesized secondary amines had TDP1 inhibitory activity IC50 in the range of 0.79-9.2 µM. The highest activity was found for (–)-myrtenal derivatives containing p-bromoaniline or m-(trifluoromethyl)aniline residue. Conclusion: We synthesized 22 secondary amines; of these, 17 amines are novel chemical structures. Many of the amines inhibit TDP1 activity in the low micromolar range. Therefore, these compounds are promising for further study of their antiproliferative activity in conjunction with DNA damaging drugs.


Author(s):  
A.V. Kovtun ◽  
◽  
S.A. Varenichenko ◽  
E.V. Zaliznaya ◽  
A.V. Mazepa ◽  
...  

We have proposed a method for the synthesis of previously unknown bromo xanthenes using the reagent PBr3/DMF as a rearrangement initiator. Bromo derivatives of xanthenes in the form of organic perchlorates were prepared by reacting the corresponding benzo(naphtho)dioxin-4(1)-ones with a three-fold excess of Vilsmeier-Haack PBr3/DMF reagent at 1100C for 2 hours, followed by the addition of sodium perchlorate. The conditions for the synthesis of formyl derivatives of xanthenes under conditions of acid hydrolysis were selected. The structure of the compounds was confirmed by 1H and 13C NMR spectral data and mass spectrometry. Preliminary studies showed that it is possible to selectively replace the dimethylamino group and the bromine atom with various nucleophiles in bromo derivatives of xanthenes, which opens up wide possibilities for the synthesis of low-molecular building blocks and dyes.


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