Artículos

New Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors Show Low Nanomolar Inhibition of Single and Double HIV-1 Mutant Strains

We designed and synthesized 21 new indolylarylsulfones (IASs) as new HIV-1 NNRTIs. Among these, IAS 12 exhibited a remarkable antiviral activity against single and double mutants (K103N EC50 = <0.7 nM; Y181C EC50 = <0.7 nM; Y188L EC50 = 21.3 nM; K103N-Y181C EC50 = 6.2 nM), resulting equally or more active than previuosly reported IAS 6 and some approved anti-HIV-1 drugs.

Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones

Conformational restriction applied to dihydrobenzylpyrimidin-4-(3 H)-ones (DABOs) by the intoduction of a methyl group at the α-benzylic position is known to massively improve the anti-HIV-1 activity of these compounds. Here, we report the effects of methoxy substitution at the α-benzylic position in S-, NH-, and N, N-DABOs carrying 2,6-difluoro, 2-chloro-6-fluoro, or 2,6-dichloro substituted benzyl moieties.

Identification of Broad-Spectrum Dengue/Zika Virus Replication Inhibitors by Functionalization of Quinoline and 2,6-Diaminopurine Scaffolds

Social and demographic changes across the world over the past 50 years have resulted in significant outbreaks of arboviruses such as dengue virus (DENV) and Zika virus (ZIKV). Despite the increased threat of infection, no approved drugs or fully protective vaccines are available to counteract the spread of DENV and ZIKV. The development of "broad-spectrum" antivirals (BSAs) that target common components of multiple viruses can be a more effective strategy to limit the rapid emergence of viral pathogens than the classic "one-bug/one-drug" approach.

Inoculantes microbianos comerciales con PGPR sobre variables productivas y económicas de fríjol común (Phaseolus vulgaris L.)*

En la provincia de Loja en las zonas de Chaguarpamba, Lozumbe y Hacienda Cristal, se colectaron de forma aleatoria muestras de suelo en plantas de café. Para el aislamiento de los microorganismos rizosféricos se realizaron diluciones seriadas hasta 10-5 y se sembraron por triplicado en placas de Petri con agar nutriente para el crecimiento de los microorganismos, se incubaron a 28 ºC durante 72 horas.

Caracterización morfológica y fisiológica de microorganismos rizosféricos nativos de sistemas agroforestales de café

En la provincia de Loja en las zonas de Chaguarpamba, Lozumbe y Hacienda Cristal, se colectaron de forma aleatoria muestras de suelo en plantas de café. Para el aislamiento de los microorganismos rizosféricos se realizaron diluciones seriadas hasta 10-5 y se sembraron por triplicado en placas de Petri con agar nutriente para el crecimiento de los microorganismos, se incubaron a 28 ºC durante 72 horas.

Caracterización morfológica de hongos micorrízicos arbusculares (HMA) asociados al café en sistemas agroforestales de la provincia de Loja, Ecuador

Los Hongos Micorrízicos Arbusculares (HMA) son de importancia en la rizósfera, puesto que, establecen simbiosis con aproximadamente el 80 % de las plantas, dicha asociación coadyuva a una mejor absorción de agua y nutrientes, así como a proteger al sistema radicular de las plantas; es así que los HMA se encuentran en todos los tipos de suelo, presentando alto potencial como biofertilizantes en los diferentes cultivos.

Dinuclear Iron Complexes of Iminopyridine-Based Ligands as Selective Cytotoxins for Tumor Cells and Inhibitors of Cancer Cell Migration

A family of dinuclear iron (II) compounds with iminopyridine-based ligands displays selective cytotoxic activity against cancer cell lines. All compounds have IC50 values 2–6 fold lower than that of cisplatin, and 30–90 fold lower than that of carboplatin for the tumor cell lines assayed. Comparing the IC50 values between tumor and non-tumor cell lines, the selectivity indexes range from 3.2 to 34, compound 10, [Fe2(4)2(CH3CN)4](BF4)4, showing the highest selectivity.

A Nuclear-Directed Ribonuclease Variant Targets Cancer Stem Cells and Inhibits Migration and Invasion of Breast Cancer Cells

During the past decades the achievements made in treating cancers have significantly improved the survival of patients. However, cancer is still one of the leading causes of mortality. It is suggested that treatment failure is mediated by a subpopulation of tumor cells named cancer stem cells that can survive after treatment and promote cancer relapse. Targeting these cells is important to improve cancer therapy. The aim of our study is to determine the effect of a human ribonuclease variant on breast cancer cells grown in 3D and on cancer stem cells.

0