A series of 2-pyrazolines 5-9 have been synthesized from α,β-unsaturated ketones 2-4. New 2-pyrazoline derivatives 13-15 bearing benzenesulfonamide moieties were then synthesized by condensing the appropriate chalcones 2-4 with 4-hydrazinyl benzenesulfonamide hydrochloride. Ethyl [1,2,4] triazolo[3,4-c][1,2,4]triazino[5,6-b]-5H-indole-5-ethanoate (26) and 1-(5H-[1,2,4]triazino[5,6-b] indol-3-yl...

STAT3 and Akt signaling have been validated as potential molecular targets for treatment of cancers including melanoma. These small molecule inhibitors of STAT3 or Akt signaling are promising for developing anti-melanoma therapeutic agents. MLS-2438, a novel 7-bromoindirubin, a derivative of the natural product indirubin, was synthesized with a bromo-group at the 7-position on one indole ring a...

A newly synthesized indole-derivative is able to induce cytostatic and cytotoxic effects in the colon cancer cells HT29, effecting apoptosis by activation of an intrinsic pathway. Magnesium is involved in both cell growth and apoptosis even though its role in the latter process is not well defined. The aims of this work were: firstly, to verify if magnesium content is related to the proliferati...

Thirteen heterocyclic quinones (5 quinoline quinones, 7 isoquinoline quinones, 1 indole quinone) were tested for their effects on avian myeloblastosis virus reverse transcriptase, growth of murine lymphoblastoma L5178Y cells, respiration of rat liver mitochondria and oxidation of NADH by Clostridium kluyveri diaphorase in comparison with those of streptonigrin, in which the quinoline quinone mo...

Indolylimidazole ring-containing natural and synthesized compounds have shown vast biological activities. These indolylimidazole contain both indole imidazole rings. The structure resembling 1a-1d 2a-2d were by a green efficient one-pot four components condensation of indole-3-carbaldehyde, benzil, ammonium-acetate, substituted amines under microwave irradiation using Amberlyst A-15 as recyclab...

The Solvatochromic technique was used to examine the solvent effects of ethyl 5-methyl-3 phenyl-1 H -indole 2-carboxylate [5-MPIC]. Different solvents were record 5-MPIC’s absorption and emission spectra at room temperature (300 K). ground state excited dipole moments estimated experimentally using Lippert’s, Bakshiev’s Kawaski Chamma Viallet’s equations. HOMO-LUMO gap MEP map also theoreticall...

Jasmonate (JA) is an important plant stress hormone that induces various plant defense responses, including the biosynthesis of protective secondary metabolites. The induction of the secondary metabolite biosynthetic gene Strictosidine synthase (Str) in Catharanthus roseus (periwinkle) cells by elicitor requires JA as a second messenger. A 42 bp region in the Str promoter is both necessary and ...

Degradation of tryptophan to indole, pyruvate, and ammonia by tryptophanase (EC 4....) from Escherichia coli, previously thought to be an irreversible reaction, is readily reversible at high concentrations of pyruvate and ammonia. Tryptophan and certain of its analogues, e.g., 5-hydroxytryptophan, can be synthesized by this reaction from pyruvate, ammonia, and indole or an appropriate derivativ...

In order to improve the production of the anticancer dimeric indole alkaloids in Catharanthuse roseus, much research has been dedicated to culturing cell lines, hairy roots, and efforts to elucidate the regulation of the monoterpenoid indole alkaloid (MIA) biosynthesis. In this study, the ORCA3 (Octadecanoid-derivative Responsive Catharanthus AP2-domain) gene alone or integrated with the G10H (...