A series of novel potential DNA bis-intercalators were designed and synthesized, in which two glucuronic acids were linked by ethylenediamine, and the glucuronic acid was coupled with various chromophores, including quinoline, acridine, indole and purine, at the C-1 position. The preliminary binding properties of these compounds to calf thymus DNA (CT-DNA) have been investigated by UV-absorptio...

Starting from L-aspartic acid the preparation of 8-aminopyrido[1,2-a]indole derivatives as benzo-fused analogs of the dopamine autoreceptor agonist 1 is reported. The key step of the synthesis is the Tf2O induced cyclization of the 1,2-amino alcohol 6. Receptor binding studies indicated selective affinity for the D-2 autoreceptor. Among the tested compounds, the dipropylamino derivative 2 showe...

Indomethacin is an indole-3-acetic acid derivative (Fig. 1), which has been shown by animal experiments to possess powerful anti-inflammatory and anti-pyretic properties without evidence of toxicity other than causing diarrhoea and gastro-intestinal irritation when given in excessive dosage (Hodgkinson, 1963). Preliminary reports of its action in arthritic patients have been given at the Americ...

Indole derivatives including bromoindoles have been isolated from the South Pacific marine sponges Rhopaloeides odorabile and Hyrtios sp. Their structures were established through analysis of mass spectra and 1D and 2D NMR spectroscopic data. Their potential inhibitory phospholipase A₂ (PLA₂), antioxidant and cytotoxic activities were evaluated. The new derivative 5,6-dibromo-L-hypaphorine (9) ...

The photophysics of the dye Lucifer Yellow ethylenediamine (LYen) has been investigated in various polar solvents. The main deactivation pathways of its first singlet excited state are the fluorescence and the intersystem crossing. In water, non-radiative decay by intermolecular proton transfer becomes a significant deactivation channel. The early fluorescence dynamics, which was investigated i...

The reaction of 6-amino-1,3-dimethylpyrimidine-2,4(1H,3H)-dione (1) as a binucleophile with primary aromatic or heterocyclic amines and formaldehyde or aromatic (heterocyclic) aldehydes in a molar ratio (1:1:2) gave the pyrimido[4,5-d]pyrimidin-2,4-dione ring systems 2-5. Treatment of 1 with diamines and formalin in molar ratio (2:1:4) gave the bis-pyrimido[4,5-d]pyrimidin-2,4-diones 6-8. Furth...

Biological screening of (hetero)aromatic compounds allowed the identification of some novel inhibitors of Abeta(1-40) aggregation, bearing indane and indole rings as common scaffolds. Molecular decoration of lead compounds led to inhibitors exhibiting a potency, measured by the Thioflavin T fluorimetric assay, ranging from high to low micromolar IC(50). The 2-(p-isopropylphenyldiazenylmethylene...

The title compound, C(23)H(18)N(2)O(2)·0.5H(2)O, a derivative of the biologically active compound curcumin, crystallizes with two organic mol-ecules and a solvent water mol-ecule in the asymmetric unit. Each of the two independent mol-ecules is close to being planar (the dihedral angles between the indole ring systems are approximately 9 and 12°) and each exists in the keto-enol form. There is ...

Reaction of 4-anthracen-9-yl-4-oxo-but-2-enoic acid (1) with indole gave the corresponding butanoic acid 2. Cyclocondensation of 2 with hydrazine hydrate, phenyl hydrazine, semicarbazide and thiosemicarbazide gave the pyridazinone derivatives 3a-d. Reaction of 3a with POCl(3) for 30 min gave the chloropyridazine derivative 4a, which was used to prepare the corresponding carbohydrate hydrazone d...

A series of indole (In) and carbazole (Cz) derivative monomers have been synthesized, such as 4-[3-carbazolyl] (4In-3Cz), 5-[3-carbazolyl] (5In-3Cz), 6-[3-carbazolyl] (6In-3Cz), 7-[3-carbazolyl] (7In-3Cz). The comonomers synthesized by Stille coupling reaction were characterized 1H-NMR elemental analysis. Potentiodynamic method was used for electropolymerization comonomers, Indole, Cz, the mixt...