Ricerc@Sapienza

A multi-component Povarov reaction was used for the preparation of [4], [5] and [6]aza- and azaoxahetero helical-shaped compounds. The oxidation of the tetrahydroquinolinic primary Povarov adducts to the aromatic quinolines is mandatory to achieve a helical-shaped structure and can be carried out in a one-pot fashion with DDQ. Resolution of [5] and [6]heterohelicenes was successfully performed by chiral HPLC.

Commercially available pesticides were examined as Mus musculus and Homo sapiens acetylcholinesterase (mAChE and hAChE) inhibitors by means of ligand-based (LB) and structure-based (SB) in silico approaches. Initially, the crystal structures of simazine, monocrotophos, dimethoate, and acetamiprid were reproduced using various force fields. Subsequently, LB alignment rules were assessed and applied to determine the inter synaptic conformations of atrazine, propazine, carbofuran, carbaryl, tebufenozide, imidacloprid, diuron, monuron, and linuron.

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials, which are published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules [...].

In this paper, we describe a small library of easy-to-prepare chiral (cyclopentadienone)iron pre-catalysts for enantioselective C[dbnd]O and C[dbnd]N hydrogenations. Starting from readily accessible achiral materials, six chiral (cyclopentadienone)iron complexes (1a-f) possessing a stereogenic plane were synthesized in racemic form. Based on the screening of pre-catalysts (±)-1a-f in the hydrogenation of ketones and ketimines, we selected two complexes (1a and 1d) for resolution by semipreparative enantioselective HPLC.

In this work the HPLC and NMR analysis of the phenyl-ethanoid glycosides (PhGs) pattern of a cultivated exemplar of Verbascum thapsus L. (Scrophulariaceae) from the Etnean area (Sicily, Italy) was performed in order to verify their possible presence. Wild V. thapsus is well-known in ethnopharmacology due to the several beneficial effects that it is able to exert and which are primarily due to these compounds. So, it’s extremely important that also cultivated exemplars of this species biosynthesize them in order to maintain their pharmacological properties.

Painting and body art are increasing their utilisation as well as their cultural impact, since piercing and tattoos are expanding social phenomena, involving many young people. However, the utilised materials often enter the market with insufficient control and several cases of skin damages are reported. Safety of the utilised products must be ensured by adequate quality controls which must be easily made, rapid, low cost, clear and persuasive.

Lamiaceae (or Labiatae) is a family of plants included in the Angiosperms group comprising 12 subfamilies, 16 tribes, 9 subtribes, 236 genera, and more than 7000 species. It represents what is probably one of the best-known and most-studied families from the phytochemical and ethnopharmacological standpoints, because it contains several compounds with great relevance and many important biological properties. In the context of phytochemistry, Lamiaceae can be unofficially divided into two major groups.

DNA is an entity shielded by mechanisms that maintain genomic stability and are essential for living cells; however, DNA is constantly subject to assaults from the environment throughout the cellular life span, making the genome susceptible to mutation and irreparable damage. Cells are prepared to mend such events through cell death as an extrema ratio to solve those threats from a multicellular perspective. However, in cells under various stress conditions, checkpoint mechanisms are activated to allow cells to have enough time to repair the damaged DNA.

c-MET pathway over-activation is the signature of malignancy acquisition or chemotherapy resistance of many cancers. We recently demonstrated that type II Testicular Germ Cell Tumours (TGCTs) express c-MET receptor. In particular, we elucidated that the non-seminoma lesions express c-MET protein at higher level, compared with the seminoma ones. In line with this observation, NTERA-2 clone D1 (NT2D1) non-seminoma cells increase their proliferation, migration and invasion in response to Hepatocyte Growth Factor (HGF).