β-Carboline derivatives are potent against Acute Myeloid Leukemia in vitro and in vivo.

Background: β-carboline alkaloids exert a distinguished ability to impair cell growth and induce cell death in a variety of cancers and the evaluation of such new therapeutic candidates may denote new possibilities for leukemia treatment. In this present study, we screened 12 β-carboline derivatives containing different substituents at 1- and 3-positions of β-carboline nucleus for their antineoplastic activities in a panel of leukemia cell lines.

Methods: The cytotoxic effects of the β-carboline derivatives were evaluated in different leukemia cell lines as well as reactive oxygen species (ROS) generation, autophagy, and important signaling pathways.

Sensitizing agents found in children and adolescents with recalcitrant atopic dermatitis: a cross-sectional study with a pediatric battery.

Background: Atopic dermatitis is the most common inflammatory skin disease in childhood and has an important impact on quality of life, especially severe cases or those that are recalcitrant to treatments. Sensitization to allergens with the potential for allergic contact dermatitis is a factor associated with cases of recalcitrant atopic dermatitis. Understanding the relationship between atopic dermatitis, allergens, and allergic contact dermatitis is essential.

β-carbolines RCC and C5 induce the death of intracellular amastigotes.

Cutaneous leishmaniasis is caused by spp., and its treatment is limited. The β-carbolines have shown activity against kinetoplastids.

Novel arylcarbamate-N-acylhydrazones derivatives as promising BuChE inhibitors: Design, synthesis, molecular modeling and biological evaluation.

A novel series of arylcarbamate-N-acylhydrazones derivatives have been designed and synthesized as potential anti-cholinesterase agents. In vitro studies revealed that these compounds demonstrated selective for butyrylcholinesterase (BuChE) with potent inhibitory activity. The compounds 10a-d, 12b and 12d were the most potent BuChE inhibitors with IC values of 0.

Membrane dynamics in Leishmania amazonensis and antileishmanial activities of β-carboline derivatives.

Two β-carboline compounds, 8i and 6d, demonstrated in vitro antileishmanial activity against Leishmania (L.) amazonensis promastigotes similar to that of miltefosine (MIL). Estimates of the membrane-water partition coefficient (K) and the compound concentrations in the membrane (c) and aqueous phase (c) for half maximal inhibitory concentration were made.

Synthesis, antileishmanial activity and mechanism of action studies of novel β-carboline-1,3,5-triazine hybrids.

A series of novel hybrids β-carboline-1,3,5-triazine were synthesized and evaluated for their in vitro antileishmanial activity against promastigote and amastigote forms of Leishmania amazonensis. Among the compounds tested, the hybrids 9d, 9e, 16a and 16b showed potent activity against the promastigote forms with IC values less than 8 μM. Compounds 9e and 16b were also active against amastigote forms, displaying IC values of 1.

Synthesis and evaluation of novel hybrids β-carboline-4-thiazolidinones as potential antitumor and antiviral agents.

A series of novel hybrids β-carboline-4-thiazolidinones were synthesized and evaluated for their in vitro antitumor activity against human cancer cell lines and for antiviral activity towards Herpes simplex virus type-1 (HSV-1). From the N'-(2-ylidene-4-thiazolidinone)-β-carboline-3-carbohydrazide series (9-11), compounds 9c and 11d were the most active, showing growth inhibition 50% (GI) values less than 5 μM for all cell lines tested. Compound 9c, bearing the 4-dimethylaminophenyl group at C-1 of β-carboline was selected for further investigation concerning cell death and cell cycle profile, focusing on the human renal adenocarcinoma cell line 786-0.