Continuing efforts to discover novel means of combating fluconazole resistance in Candida albicans have identified an indole derivative that sensitizes strains demonstrating resistance to fluconazole. This tetracycle (3, ML229) does not appear to act through established Hsp90 or calcineurin pathways to chemosensitize C. albicans, as determined in Saccharomyces cerevisiae models, and may be a us...

Herein we report the de novo design and synthesis of a geometrically flexible bis-indole carboxamide and a constrained derivative, as a novel class of small molecule scaffold that exhibits high stabilization potential for DNA G-quadruplex sequences associated with the promoters of c-kit2 and c-myc.

The Stille coupling reaction of the stannylindole 13 with the 5-iodoimidazole derivative 14 (or 27) in the presence of PdCl(2)(PPh(3))(2) gave the corresponding indole-imidazole coupling product 15 (or 28), thereby affording a synthetic approach to 10-methylgranulatimide (7), 15-methylgranulatimide (11), and 10, 15-dimethylgranulatimide (12), as well as 10-methylisogranulatimide B (5).

The violet pigment violacein is an indole derivative, isolated mainly from bacteria of the genus Chromobacterium, which exhibits important antitumoral, antimicrobial and antiparasitary properties. Furthermore, the formulation of violacein in different polymeric carriers developed so far offers alternative approaches to overcoming physiological barriers and undesirable physicochemical properties...

Rebeccamycin derivative 1 bearing a sugar moiety linked to both indole nitrogens and an amino substituent on the carbohydrate unit was synthesized in three steps from the bacterial metabolite. This compound was found to be a highly potent checkpoint kinase 1 inhibitor with an IC(50) value of 2.8nM.

We describe the utility of a Pd/C-Cu mediated method in the synthesis of 2,5-disubstituted indoles in water via a coupling-cyclization strategy. Further application of this methodology has been demonstrated in the preparation of a target indole derivative via a 7-step process the key step being the Pd/C-mediated coupling reaction.

Lead tetraacetate oxidation of a Corynanthe-type indole alkaloid, mitragynine, produced mainly 7-acetoxyindolenine derivative (2) together with a dimeric compound (4) as a minor product. The novel structure having a bridge between the C-11' and C-7 positions in the respective indolenine parts and its formation mechanism were studied.

The radioprotective ability of L-tryptophan, tryptamine, 3-indoleacetic and indole (10~4 m), on UV and gamma irradiated DNA (10-4 m) is studied. UV radioprotection is accomplished in the following order of efficiency: L-Tryptophan and 3-indoleacetic acid > indole and tryptamine. The corresponding DRF measured as absorbancy loss at 260 nm, were: L-Tryptophan and 3-indoleacetic acid around 3 and ...

When Escherichia coli K-12 is grown anaerobically in medium containing tryptophan and sodium nitrate, it produces red compounds. The reaction requires functional genes for trytophanase (tnaA), a tryptophan permease (tnaB), and a nitrate reductase (narG), as well as a natural drop in the pH of the culture. Mass spectrometry revealed that the purified chromophores had mass/charge ratios that clos...

Abstract Background In medicinal chemistry, indole and its derivative play an important role. Indole is gaining a lot of importance in chemistry due to physiological activity which includes anticancer, antitubercular, antimicrobial, antiviral, antimalarial, anti-inflammatory activities, antileishmanial agents, anti-cholinesterase, enzyme inhibitory. The spread antimicrobial resistance becomes t...