19126-12-6Relevant academic research and scientific papers
Synthesis of novel proxyphylline derivatives with dual Anti-Candida albicans and anticancer activity
Borowiecki, Pawe?,Wińska, Patrycja,Bretner, Maria,Gizińska, Ma?gorzata,Koronkiewicz, Miros?awa,Staniszewska, Monika
, p. 307 - 333 (2018/03/21)
Three out of 16 newly synthesized 1,3-dimethylxanthine derivatives (proxyphylline analogues) exhibited consistencies between antifungal and anticancer properties. Proxyphylline possessing 1-(10H-phenothiazin-10-yl)propan-2-yl (6) and polybrominated benzimidazole (41) or benzotriazole moiety (42) remained selectively cidal against Candida albicans (lg R ≥ 3 at conc. of 31, 36 and 20 μM, respectively) however not against normal mammalian Vero cell line in vitro (IC50 ≥ 280 μM) and Galleria mellonella in vivo. These compounds also displayed moderate antineoplastic activity against human breast adenocarcinoma (MCF-7) cell line (EC50 = 80 μM) and high against peripheral blood T lymphoblast (CCRF-CEM) (EC50 = 6.3–6.5 μM). In addition, 6 and 42 exerted: (1) dual activity against fungal adhesion and damage mature biofilm; (2) necrosis of planktonic cells due to loss of membrane function and of structural integrity; (3) biochemical (inhibition of sessile cell respiration) and morphological changes in cell wall polysaccharide contents. Therefore, leading proxyphylline derivatives can be employed to prevent cancer-associated biofilm Candida infections.
Chiral N-heterocyclic carbene ligands for asymmetric catalytic oxindole synthesis
Jia, Yi-Xia,Hillgren, J. Mikael,Watson, Emma L.,Marsden, Stephen P.,Kuendig, E. Peter
supporting information; scheme or table, p. 4040 - 4042 (2009/03/11)
The Pd-catalysed asymmetric intramolecular α-arylation of amide enolates containing heteroatom substituents gives chiral 3-alkoxy or 3-aminooxindoles in high yield and with enantioselectivities up to 97% ee when a new chiral N-heterocyclic carbene ligand is used. The Royal Society of Chemistry.
Conformational Structure and Dynamics of Arylmethoxyacetates: DNMR Spectroscopy and Aromatic Shielding Effect
Latypov, Sh. K.,Seco, J. M.,Quinoa, E.,Riguera, R.
, p. 504 - 515 (2007/10/02)
The ground state conformational geometry and energy of esters of (R)- and (S)-arylmethoxyacetic acids were evaluated from low temperature 1H and 13C NMR spectra and by means of MM, AM1, and aromatic shielding effect calculations.In solution, the title com
