38667-55-9Relevant academic research and scientific papers
Proliferation inhibition of novel diphenylamine derivatives
Janovec, Ladislav,Jano?ková, Jana,Matejová, Mária,Konko?ová, Eva,Paulíková, Helena,Lichancová, Daniela,Júno?ová, Lenka,Hamu?aková, Slávka,Imrich, Ján,Ko?urková, Mária
, p. 487 - 499 (2019)
Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most widely used drugs in the world but some NSAIDs such as diclofenac and tolfenamic acid display levels of cytotoxicity, an effect which has been attributed to the presence of diphenylamine contained in their structures. A novel series of diphenylamine derivatives were synthetised and evaluated for their cytotoxic activities and proliferation inhibition. The most active compounds in the cytotoxicity tests were derivative 6g with an IC50 value of 2.5 ± 1.1 × 10?6 M and derivative 6f with an IC50 value of 6.0 ± 3.0 × 10?6 M (L1210 cell line) after 48 h incubation. The results demonstrate that leukemic L1210 cells were much more sensitive to compounds 6f and 6g than the HEK293T cells (IC50 = 35 × 10?6 M for 6f and IC50 > 50 × 10?6 M for 6g) and NIH-3T3 (IC50 > 50 × 10?6 M for both derivatives). The IC50 values show that these substances may selectively kill leukemic cells over non-cancer cells. Cell cycle analysis revealed that a primary trend of the diphenylamine derivatives was to arrest the cells in the G1-phase of the cell cycle within the first 24 h. UV–visible, fluorescence spectroscopy and circular dichroism were used in order to study the binding mode of the novel compounds with DNA. The binding constants determined by UV–visible spectroscopy were found to be in the range of 2.1–8.7 × 104 M?1. We suggest that the observed trend for binding constant K is likely to be a result of different binding thermodynamics accompanying the formation of the complexes.
Novel trisubstituted acridines as human telomeric quadruplex binding ligands
Ungvarsky, Jan,Plsikova, Jana,Janovec, Ladislav,Koval, Jan,Mikes, Jaromir,Mikesová, Lucia,Harvanova, Denisa,Fedorocko, Peter,Kristian, Pavol,Kasparkova, Jana,Brabec, Viktor,Vojtickova, Maria,Sabolova, Danica,Stramova, Zuzana,Rosocha, Jan,Imrich, Jan,Kozurkova, Maria
, p. 13 - 29 (2014/11/07)
A novel series of trisubstituted acridines were synthesized with the aim of mimicking the effects of BRACO19. These compounds were synthesized by modifying the molecular structure of BRACO19 at positions 3 and 6 with heteroacyclic moieties. All of the derivatives presented in the study exhibited stabilizing effects on the human telomeric DNA quadruplex. UV-vis spectroscopy, circular dichroism, linear dichroism and viscosimetry were used in order to study the nature of the DNA binding in more detail. The results show that all of the novel derivatives were able to fold the single-stranded DNA sequences into antiparallel G-quadruplex structures, with derivative 15 exhibiting the highest stabilizing capability. Cell cycle analysis revealed that a primary trend of the "braco"-like derivatives was to arrest the cells in the S- and G 2M-phases of the cell cycle within the first 72 h, with derivative 13 and BRACO19 proving particularly effective in suppressing cell proliferation. All studies derivatives were less toxic to human fibroblast cell line in comparison with HT 29 cancer cell line.
Substituted benzimidazoles and imidazo-[4,5]-pyridines
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, (2008/06/13)
2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
SYNTHESIS OF p-AMINOBENZOIC ACID AND ITS HALOGEN DERIVATIVES BY LIQUID-PHASE CATALYTIC OXIDATION OF N-ACYLATED p-TOLUIDINES
Shcherbina, F. F.,Tmenov, D. N.,Lysukho, T. V.,Belous, N. P.
, p. 340 - 342 (2007/10/02)
By the liquid-phase catalytic oxidation of N-acetyl-p-toluidine and its halogen derivatives with oxygen at atmospheric pressure the corresponding N-acetyl-p-aminobenzoic acids were obtained with yields of 95 - 97 molepercent.
