A Novel N-Tert-Butyl Derivatives of Pseudothiohydantoin as Potential Target in Anti-Cancer Therapy

Tumors are currently more and more common all over the world; hence, attempts are being made to explain the biochemical processes underlying their development. The search for new therapeutic pathways, with particular emphasis on enzymatic activity and its modulation regulating the level of glucocorticosteroids, may contribute to the development and implementation of new therapeutic options in the treatment process. Our research focuses on understanding the role of 11β-HSD1 and 11β-HSD2 as factors involved in the differentiation and proliferation of neoplastic cells. In this work, we obtained the 9 novel N-tert-butyl substituted 2-aminothiazol-4(5H)-one (pseudothiohydantoin) derivatives, differing in the substituents at C-5 of the thiazole ring. The inhibitory activity and selectivity of the obtained derivatives in relation to two isoforms of 11β-HSD were evaluated. The highest inhibitory activity for 11β-HSD1 showed compound 3h, containing the cyclohexane substituent at the 5-position of the thiazole ring in the spiro system (82.5% at a conc. 10 µM). On the other hand, the derivative 3f with the phenyl substituent at C-5 showed the highest inhibition of 11β-HSD2 (53.57% at a conc. of 10 µM). A low selectivity in the inhibition of 11β-HSD2 was observed but, unlike 18β-glycyrrhetinic acid, these compounds were found to inhibit the activity of 11β-HSD2 to a greater extent than 11β-HSD1, which makes them attractive for further research on their anti-cancer activity.     

Octacyanidorhenate(V) Ion as an Efficient Linker for Hysteretic Two-Step Iron(II) Spin Crossover Switchable by Temperature,Light, and Pressure

A two-step hysteretic Fe^II spin crossover (SCO) effect was achieved in programmed layered Cs{[Fe(3-CNpy)₂][Re(CN)₈]}⋅H₂O ( 1 ) (3-CNpy=3-cyanopyridine) assembly consisting of cyanido-bridged Fe^II-Re^V square grid sheets bonded by Cs⁺ ions. The presence of two non-equivalent Fe^II sites and the conjunction of 2D bimetallic coordination network with non-covalent interlayer interactions involving Cs⁺, [Re^V(CN)₈]³⁻ ions, and 3-CNpy ligands, leads to the occurrence of two steps of thermal SCO with strong cooperativity giving a double thermal hysteresis loop. The resulting spin-transition phenomenon could be tuned by an external pressure giving the room-temperature range of SCO, as well as by visible-light irradiation, inducing an efficient recovery of the high-spin Fe^II state at low temperatures. We prove that octacyanidorhenate(V) ion is an outstanding metalloligand for induction of a cooperative multistep, multiswitchable Fe^II SCO effect.     

A look at multiparticle production via modified combinants

The European Physical Journal A - The transverse momentum ($$p_{T}$$) distribution of strange hadrons ($$K_{S}^{0}$$ and $$\varLambda $$) and multi-strange hadrons( $$\varXi $$ and $$\varOmega $$)...     

Experimental investigation of convective mass/heat transfer in short minichannel at low Reynolds numbers

An experimental investigations of convective mass/heat transfer in short circular channel with small inner diameter at Re numbers ranging from 20 to 250 were performed. Mean values of convective mass transfer coefficients were measured using electrochemical technique – limiting current method. The results of dimensionless mass transfer coefficient Sh were compared with conventional theory. It was observed the increase of experimental Sh in compare with data from classical correlation relative to channels of conventional size. The heat transfer correlation was obtained on the basis of mass/heat transfer analogy. Chilton–Colburn analogy was applied. The effects were compared with the available literature experimental thermal balance results.     

Cyrtologies of Convergences,I

We study the complete lattice of convergences, that is, of relations between a set and the set of its filters. Various properties of convergences (like isotonicity, antitonicity, being a pseudotopology, a pretopology, an adherence) determine subsets of the lattice of convergences which possess certain particular features called “cyrtological”. The morphisms associated to these sets, said “cyrtomorphisms”, are basic in the study of convergences. A method of generation of GALOIS connections relative to cyrtomorphisms is proposed. Semigroups generated by some cyrtomorphisms are analyzed.     

The kinetics of oxiranes addition to bis/2-hydroxyalkyl/disulfides and bis/2-hydroxyalkyl/sulfides in the presence of N,N-dimethylcyclohexylamine

Rate constants for the reaction of oxiranes with bis/2-hydroxyalkyl/disulfides, bis/2-Hydroxyalkyl/sulfides, and 1,6-Hexanediol in the presence of N,N-dimethylcyclohexylamine were studied at the temperature range of 50–90°C. A mechanism of these reactions has been proposed and its kinetic equation has been presented.