New tetracyclic benzofurocoumarin (benzopsoralen) analogues were synthesized and their inhibitory effect on the growth of tumor cell lines was evaluated. The human tumor cell lines used were MDA MB231 (breast adenocarcinoma), HeLa (cervix adenocarcinoma) and TCC-SUP (bladder transitional cell carcinoma). The in vitro antitumor activity of the new benzopsoralens was discussed in terms of structure–activity relat...
Psoralens are natural products present in several plant families that are extremely toxic to a wide variety of prokaryotic and eukaryotic organisms. They are potentially active in diseases such as vitiligo, psoriasis, and several types of cancer. Following our interest on this type of compounds 1 four new psoralen analogues were prepared, 1a-1c and 1e. To synthesize 1a (R = H) the method of Harayama and Ishii w...
Tacrine is an acetylcholinesterase inhibitor used as cognitive enhancer in Alzheimer's disease treatment. However, the low therapeutic efficiency and the high incidence of side effects have limited its clinical use. In the present study, the molecular mechanisms underlying the brain activity of tacrine and two novel tacrine analogues (T1, T2) were approached focusing on three aspects: i) effects on brain cholin...
Novel psoralen analogues based on carbazoles were synthesized and characterized.
We describe the synthesis of 3H-benzofuro[3,2-f]chromen-3-ones. The anti-proliferative effect on human cancer cell lines (MDA-MB231 and HeLa) was evaluated.
4,5,6-Trimethoxyisatin was crystallized from water to give dark red needles that were characterized by NMR and IR spectroscopy, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), single-crystal X-ray diffraction (XRD) and hot-stage microscopy.
Synthesis of eleven tacrine analogues derived from N-aryl-5-amino-4-cyanopyrazoles, by a Friedländer type reaction, is described. Their structures were confirmed by 1H and 13C NMR spectroscopy, elemental analysis and/or mass spectrometry.
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