The cylcooxygenase isoforms COX‐1 and COX‐2 are involved in the production of prostaglandins physiological pathological processes. overexpression under inflammatory conditions as well its role cancer neurodegenerative diseases necessitates need to develop improve non‐steroidal anti‐inflammatory drugs. These COX inhibitors used reduce symptoms inflammation, with aspirin, indomethacin or flurbiprofen being prominent examples. To unwanted side effects connected unselective inhibition,...

Abstract Eight‐membered cyclic functional bisphosphines, namely 1,5‐di‐aryl‐3,7‐di(2‐pyridyl)‐1,5‐diaza‐3,7‐diphosphacyclooctanes (aryl=2‐pyridyl, m ‐tolyl, p diphenylmethyl, benzyl, ( R )‐(+)‐(α‐methyl)benzyl), with 2‐pyridyl substituents on the phosphorus atoms have been synthesized by condensation of 2‐pyridylphosphine, formaldehyde, and corresponding primary amine. The structures some these bisphosphines investigated X‐ray crystallography. readily form neutral P,P‐chelate complexes [(κ 2...

Abstract Enantiomerically pure ( R P , )‐ and S )‐1,2‐bis[1‐adamantyloxy‐(–)‐menthyloxyphosphanyl]‐ closo ‐dicarbaborane(12), 1,2‐bis[bis(–)‐menthyloxyphosphanyl]‐ ‐dicarbaborane(12)and 1,2‐bis[bis(4‐ tert ‐butylphenyloxy)phosphanyl]‐ ‐dicarbaborane(12) were synthesised by the reaction of dilithiated 1,2‐dicarba‐ ‐dodecaborane(12) with two equivalents corresponding chlorophosphite. The phosphonites are stable towards epimerisation, oxygen water. ··· through‐space coupling was observed, 3 J...

Abstract Dehydrocoupling of the ferrocenylphosphine–borane adducts [FcPH 2 (BH 3 )] ( 1 ) [Fc = Fe(C 5 H )(C 4 and [FcCH PH with [{Rh(μ‐Cl)(cod)} ] (cod 1,5‐cyclooctadiene) as catalyst gave corresponding phosphorus–boron‐based polymers [FcPH(BH n PH(BH low‐ (heating in toluene, low or high‐molecular‐weight without solvent, high poly(ferrocenylphosphinoborane)s depending on reaction conditions. a racemic mixture [2‐ N , ‐dimethyl( ‐borane)aminomethyl‐1‐ferrocenyl]phosphine–borane 6 resulted...

A series of racemic and optically pure aminoalkylferrocenyldichlorophosphanes has been prepared by reaction phosphorus trichloride with the corresponding lithiated aminoalkylferrocene precursors. Crystal structures 1-dichlorophosphanyl-2-N,N-dimethylaminomethylferrocene, 1-dichlorophosphanyl-2-N,N-dimethylaminomethyl-3-triphenylsilylferrocene (S)-N,N-dimethyl-1-[(R)-2-(dichlorophosphanyl)ferrocenyl]ethylamine reveal short intramolecular N⋯P distances, which are suggestive weak N → P dative...

Mefenamic acid represents a widely used nonsteroidal anti-inflammatory drug (NSAID) to treat the pain of postoperative surgery and heavy menstrual bleeding. Like other NSAIDs, mefenamic inhibits synthesis prostaglandins by nonselectively blocking cyclooxygenase (COX) isoforms COX-1 COX-2. For improved selectivity and, therefore, reduced related side effects, carborane analogues were evaluated. The ortho-, meta-, para-carborane derivatives synthesized in three steps: halogenation respective...

The luminal A-subtype of breast cancer, where the oestrogen receptor α (ERα) is overexpressed, most frequent one. prodrug tamoxifen (1) clinically used agent, inhibiting ERα activity via formation several active metabolites, such as 4-hydroxytamoxifen (2) or 4,4'-dihydroxytamoxifen (3). In this study, we present derivative 4-[1,1-bis(4-methoxyphenyl)but-1-en-2-yl]-2,2'-bipyridine (4), which was combined with platinum palladium dichloride, former a well-known scaffold in anticancer treatment,...

Organotin(IV) carboxylates are a class of compounds explored as alternatives to platinum-containing chemotherapeutics due propitious in vitro and vivo results, distinct mechanisms action. In this study, triphenyltin(IV) derivatives non-steroidal anti-inflammatory drugs (indomethacin (HIND) flurbiprofen (HFBP)) synthesized characterized, namely [Ph3Sn(IND)] [Ph3Sn(FBP)]. The crystal structure reveals penta-coordination the central tin atom with almost perfect trigonal bipyramidal geometry...

The synthesis of novel organic molecular frameworks with strong luminescence in the solid state has become an enormously growing area current research due to their versatile applications for optoelectronics or bioimaging. Here, a facile synthetic strategy via MnIII-mediated oxidative annulation reaction obtain propeller-rich molecules bearing thieno[3,2-b]phosphole motif as stator moiety is reported. All synthesized compounds show aggregation-induced emission (AIE) characteristics,...

Complexes of the type [Ru(N-N)(2)(bxbg)]Cl(2) where N-N is 2,2'-bipyridine (bpy) (1), 1,10-phenanthroline (phen) (2), dipyrido [3,2-d:2',3f] quinoxaline (dpq) (3), and dipyrido[3,2-a:2',3'-c]phenazine (dppz) (4) which incorporate bis(o-xylene)bipyridine glycoluril (bxbg) as ancillary ligand have been synthesized characterized by IR, NMR, UV-visible, luminescence, ESI-MS, cyclic voltammetry, spectroelectrochemistry. The initiates a head to association act nucleation point for further growth...

The strength of conjugation between the diene moieties 1-R-1,2-diphospholes and 1-R-phospholes exocyclic phenyl groups these P-heteroles has been quantitatively characterized by use Raman activities bands substituents. It is shown that in both types phospholes very similar to with system cyclopentadiene. Introduction substituents (−OMe, −C(═O)H, −NO2, −NMe2, −CH═CH2) para-position extends π-delocalization into electronic 1,2-diphosphole ring, producing bathochromic shifts absorption up 63...

A series of Ru(II) arene complexes mono- and bidentate N-donor ligands with carboxyl or ester groups chlorido ancillary were synthesised structurally characterised. The have a distorted tetrahedral piano-stool geometry. binding interaction was studied calf thymus DNA (CT-DNA) by absorption titration, viscosity measurement, thermal melting, circular dichroism, ethidium bromide displacement assay cleavage plasmid (pBR322), investigated gel electrophoresis. dichlorido bind covalently to in the...

Phosphole oxides undergo a highly chemoselective reaction with sulfonyl isocyanates forming sulfonylimino phospholes in high yields. This facile modification proved to be powerful tool for obtaining new phosphole-based aggregation-induced emission (AIE) luminogens fluorescence quantum yields the solid state. Changing chemical environment of phosphorus atom phosphole framework results significant shift maximum longer wavelengths.

This study explores the anti‐cancer potential of N‐methylated open‐ring derivatives carborane‐substituted diclofenac analogs. By N‐methylation, open‐chain form could be trapped and cyclization back to lactam or amidine was inhibited. A small library carborane‐ phenyl‐based secondary tertiary arylamines bearing carboxylic acid nitrile groups synthesized analyzed for their COX‐affinity in vitro silico. The compounds were further evaluated against mouse adenocarcinoma (MC38), human colorectal...

The cannabinoid receptor type 2 (CB2R) is overexpressed under pathological conditions. PET a suitable non‐invasive imaging technique for diagnosing disease states, but requires radiotracer that binds to CB2R with high affinity and selectivity. Currently, there no candidate routinely used in the clinics. naphthyridinone scaffold promising core structure has been modified past years. modification of carboxamides carboranes as hydrophobic surrogates purely organic moieties could lead beneficial...

The title compound was obtained from the cyclic diaminogermylene C(2)H(2)[N(CH(2)Bu(t))](2)Ge and cis-[Mo(CO)(4)(NCEt)(2)] its crystal structure determined revealing structural changes in coordinated ligand indicative of strong pi-acceptor properties.

The reaction of [NiBr(2)(bpy)(2)] (bpy = 2,2'-bipyridine) with organic phosphinic acids ArP(O)(OH)H [Ar Ph, 2,4,6-trimethylphenyl (Mes), 9-anthryl (Ant)] leads to the formation binuclear nickel(II) complexes bridging ArP(H)O(2)(-) ligands. Crystal structures [Ni(2)(μ-O(2)P(H)Ar)(2)(bpy)(4)]Br(2) (Ar Mes, Ant) have been determined. In each structure, metal ions distorted octahedral coordination and are doubly bridged by two arylphosphinato Magnetic susceptibility measurements shown that these...

Two novel water soluble ruthenium(II) complexes [Ru(bpy)2(bqbg)]2+ and [Ru(phen)2(bqbg)]2+ have been structurally characterized their DNA condensation activity, cytotoxicity, cellular uptake studies of condensates as potential non-viral carriers were evaluated.

Heating of a mixture [Ni(CH2═CH2)(dtbpe)] (dtbpe = 1,2-bis(di-tert-butylphosphino)ethane) and 2,6-dimesitylphenylphosphine (DmpPH2) in toluene gives the secondary phosphine (Dmp)P(Et)(H) (1) as main product. However, thermolysis [Ni(CH3)2(dtbpe)] presence DmpPH2 leads to mononuclear nickel phosphanido hydride complex [NiH{P(Dmp)(H)}(dtbpe)] (2), product an oxidative addition primary nickel(0). The structure 2 was confirmed by single-crystal X-ray diffraction DNMR studies. mutual exchange...

Abstract Modern catalysis takes advantage of aryl‐based interactions to tune and control reactions. In the design N ‐heterocyclic‐carbene catalysts, both electronic steric nature nitrogen substituents play a crucial role. Although hydrocarbon‐based systems especially aryl residues have contributed considerably overcome multifaceted catalytic challenges, unique properties carborane moieties, including delocalized charge, potential planar chirality, well‐known thermodynamic stability, offer...