Revisiting Biginelli-like reactions: solvent effects, mechanisms, biological applications and correction of several literature reports.

This study critically reevaluates reported Biginelli-like reactions using a Kamlet-Abboud-Taft-based solvent effect model. Surprisingly, structural misassignments were discovered in certain multicomponent reactions, leading to the identification of pseudo three-component derivatives instead of the expected MCR adducts. Attempts to replicate literature conditions failed, prompting reconsideration of the described MCRs and proposed mechanisms.

Correction: Exploratory comparisons between different anti-mitotics in clinically-used drug combination in triple negative breast cancer.

[This corrects the article DOI: 10.18632/oncotarget.28068.

When the tail shakes the snake: phylogenetic affinities and morphology of Atractus badius (Serpentes: Dipsadidae), reveals some current pitfalls on the snake's genomic age.

Atractus badius has a long and controversial nomenclatural history due to both its antiquity and the brevity of its original description. This species was described based on two syntypes from Java. Later, a lectotype was designated and the distribution range restricted to the Guiana Shield.

Exploratory comparisons between different anti-mitotics in clinically-used drug combination in triple negative breast cancer.

Triple-negative breast cancer (TNBC) constitutes a very aggressive type of breast cancer with few options of cytotoxic chemotherapy available for them. A chemotherapy regimen comprising of doxorubicin hydrochloride and cyclophosphamide, followed by paclitaxel, known as AC-T, is approved for usage as an adjuvant treatment for this type of breast cancer. In this study we aimed to elucidate the role of KIF11 in TNBC progression throughout its inhibition by two synthetic small molecules containing the DHPM core (dihydropyrimidin-2(1H)-ones or -thiones), with the hypothesis that these inhibitors could be an interesting option of antimitotic drug used alone or as adjuvant therapy in association with AC.

Effects of the Latex of Hook F. () on a Preclinical Model of Canine Prostate Cancer.

Prostatic cancer (PC) stands out in terms of its occurrence, pathophysiology, and unfavorable prognostics in humans and dogs. Natural drugs bear an integrative potential for conventional antineoplastic treatments. In this context, the bioproducts of have been empirically used in different parts of Brazil for the integrative treatment of prostate cancer in humans.

Synthetic enzyme-catalyzed multicomponent reaction for Isoxazol-5(4)-one Syntheses, their properties and biological application; why should one study mechanisms?

In this work, we describe the application of a synthetic enzyme (synzyme) as the catalyst to promote the multicomponent synthesis of isoxazol-5(4H)-one derivatives. The catalytic system could be used up to 15 times without any notable loss of its activity. Some derivatives showed fluorescence and their photophysical data were evaluated.

Mechanistic knowledge and noncovalent interactions as the key features for enantioselective catalysed multicomponent reactions: a critical review.

This critical review focuses on some key features which determine successful enantioselective catalysed multicomponent reactions (MCRs) and are typically underappreciated in the literature. A critical analysis of this topic is of current interest and the importance of elucidating the reaction mechanism of a MCR, which is usually a neglected task, is a feature of analysis that is aimed at successfully achieving the enantioselective version of the reaction by proper comprehension of the transformation. The key role of noncovalent interactions is another feature analysed along with the transition state (TS) of the key step for the chiral induction of some selected MCRs.

A bittersweet relationship: What does it mean to be the caregiver of a patient with bipolar disorder?

Background: As with most of the chronic illnesses, the changes and consequences brought on by bipolar disorder (BD) are not exclusive to the patient and often spread to those around them, especially for direct caregivers of these patients. It is known that there is a significant emotional and physical toll among persons who coexist daily with those who suffer from this disorder.

Objective: Aware of the importance of the role played by informal caregivers (especially the family) in the stability and evolution of patients with bipolar disorder, this study seeks to explore the perception that family members responsible for bipolar persons have of themselves as caregivers of these patients.

Osteology and Cartilaginous Elements of Trilepida salgueiroi (Amaral, 1954) (Scolecophidia: Leptotyphlopidae).

Morphological and anatomical studies on the Leptotyphlopidae have increased in the past 10 years, providing important data on the systematics of this group, mainly focused on the skull and lower jaw morphology. However, most studies are based on a single specimen, rarely combining more than one single method of assessing morphological information. Therefore, several data on postcranial morphology, sexual dimorphism, and ontogenetic and intraspecific variation of leptotyphlopids remain poorly understood.

An ionically tagged water-soluble artificial enzyme promotes the dephosphorylation reaction with nitroimidazole: enhanced ionic liquid effect and mechanism.

In this paper, we describe a novel synthesized ionically tagged water-soluble artificial enzyme (PI) that can efficiently cleave phosphate esters, with enhanced an ionic liquid effect through cooperative effects for the substrate activation and further nucleophilic reaction. The dephosphorylation reaction with PI was evaluated in the presence and absence of 2-methyl-4(5)-nitroimidazole, showing impressive rate enhancements of up to 2 × 10(6)-fold, ascribed to the imidazolide species known as excellent nucleophiles, and formed favorably at lower pH values in the presence of PI.

Impact of kinesin Eg5 inhibition by 3,4-dihydropyrimidin-2(1H)-one derivatives on various breast cancer cell features.

Background: Breast cancer is a complex heterogeneous disease and is one of the leading causes of death among women. In addressing the need for treatments of this life-threatening illness, we studied 3,4-dihydropyrimidin-2(1H)-one (or thione) derivatives (DHPMs), a class of inhibitor molecules of the Eg5 motor spindle protein that shows pronounced antitumor activity against several cancer cell lines.

Methods: An in vitro screening was performed for identification of DHPMs with potent antitumor effects on MCF-7 and MDA-MB-231 cells and the selected DHPMs were evaluated for their inhibitory activity on Eg5 both in silico, using Molecular dynamics, and in vitro Eg5 inhibition assays.

The Biginelli reaction with an imidazolium-tagged recyclable iron catalyst: kinetics, mechanism, and antitumoral activity.

The present work describes the synthesis, characterization, and application of a new ion-tagged iron catalyst. The catalyst was employed in the Biginelli reaction with impressive performance. High yields have been achieved when the reaction was carried out in imidazolium-based ionic liquids (BMI⋅PF6, BMI⋅NTf2, and BMI⋅BF4), thus showing that the ionic-liquid effects play a role in the reaction.

Morphological variation and affinities of the poorly known snake Atractus caxiuana (Serpentes: Dipsadidae) .

Atractus caxiuana was recently described based on three specimens (two males and one female) from the Floresta Nacional de Caxiuanã, municipality of Melgaço, state of Pará, in the eastern portion of the Brazilian Amazon. Apart from the type series, no additional samples are known for the species. In this study, we report new specimens of A.

Mechanistic studies on Lewis acid catalyzed Biginelli reactions in ionic liquids: evidence for the reactive intermediates and the role of the reagents.

This paper describes the use of common Lewis acids supported in imidazolium-based ionic liquids as the catalysts to promote the Biginelli reaction. The ionic liquid effect and the reaction mechanism are discussed on the basis of nuclear magnetic resonance (NMR), electrospray ionization mass spectrometry (ESI-MS), and theoretical calculations. Indeed, the results showed that the ionic medium plays a fundamental role in the synthesis of biologically active dihydropyrimidinones due to the stabilization of the charged intermediates proposed in the mechanism.

Family violence and risk of substance use among Mexican adolescents.

Objective: Determine the relationship between psychological and physical violence, exerted by fathers and/or mothers, and inter- or extra-familiar sexual violence with risk for consuming tobacco, alcohol and drugs among adolescents.

Method: A cross-sectional study was carried out with students in two secondary schools in Mexico City. A total of 936 students participated: 54.

Prevalence of codependence in young women seeking primary health care and associated risk factors.

Codependence as a relational problem that often, but not necessarily always, occurs in conjunction with familial alcoholism. Previous research has shown that various etiological factors resulting from recurring stressful circumstances experienced in childhood or adulthood may contribute to this relation. Another factor arises out of the "submission script" that may be assumed by women living within a culture that typically promotes unequal power between women and men.