The X-ray crystal structures of (2E,5E)-2-(4-cyanobenzylidene)-5-(4-dimethylaminobenzylidene)cyclopentanone (I) and (2E,5E)-2-benzylidene-5-cinnamylidenecyclopentanone (II) are presented, compared to the gas phase structures calculated using density functional theory, and discussed in the contex...

A novel N4-phenylthiosemicarbazone,3-[(E)-[(2E)-2-methyl-3-phenylprop-2-en-1-ylidene] amino]-1-phenylthiourea, abbreviated as NPCN, has been synthesized and characterized by elemental analysis and FT-IR, FT-Raman, 1H NMR, 13C NMR and electronic spectral methods. Single crystals of the title comp...

The title compound methyl(2E)-2-{[N-(2-formylphenyl)(4-methylbenzene)sulfonamido] methyl}-3-(2-methoxyphenyl)prop-2-enoate (MFMSM) has been synthesized and single crystals were grown by slow evaporation solution growth technique at room temperature. XRD, FT-IR and NMR spectra of MFMSM in the sol...

Complexes of Cu(II), Ni(II), Co(II) and Fe(II) ions with N-[2-[(hydroxyalkylimino)methyl]phenyl]-4-methylbenzenesulfonamides containing the (CH2)n-spacer of a variable length (n = 2–6) were synthesized by chemical and electrochemical methods. All the compounds were characterized by C, H and N e...

The article presents the study of psycho- and neurotropic properties of novel 3-(N-R,R′-aminomethyl)-2-methyl-1H-quinolin-4-ones in vivo. The research was carried out using the open field test, elevated plus maze, rotarod test, tail suspension test, passive avoidance test after scopolamine-indu...

For the purpose of preparation of optically active aminoalcohol congeners possessing both hydroxyl- and dialkylamino-substituted vicinal chiral carbons, lipase-assisted acylation of methyl (2E,4R*,5S*)-4-(N-benzyl-N-methyl)amino-5-hydroxyhex-2-enoate (4) using CAL-B with vinyl hexanoate as an ac...

The title compound methyl (2E)-2-{[N-(2-formylphenyl)-4-methyl benzene sulfonamido] methyl}-3-(naphthalen-1-yl) prop-2-enoate (MFMNPE) is a derivative of sulfonamide. Molecular structure and vibrational analysis of MFMNPE has been carried out by experimental and theoretical approaches. The NBO a...

The convenient synthesis of 1,5-diazaspiro[2.3]hexanes, as new structurally challenging strained diazaspirocyclic compounds, was developed starting from easily accessible ethyl 2-(bromomethyl)-1-tosylaziridine-2-carboxylate. The key transformations in the developed four-step sequence involved a ...

A novel series of aminotihazole compounds possessing phenoxy acetic acid moiety were synthesized. The synthesized compounds were evaluated for their hypolipidemic activity by using high fat diet induced hyperlipidemia in Sprague-Dawley rats.

Recent studies revealed that MALT1 is a promising therapeutic target for the treatment of ABC-DLBCL. Among several reported MALT1 inhibitors, MI-2 as an irreversible inhibitor represents a new class of ABC-DLBCL therapeutics. Due to its inherent potential cross-reactivity, further structure–act...

A series of novel 2-amino-5-chlorobenzophenone derivatives (3a–3g) were prepared by the reaction of 2-(chloroacetamido)-5-chlorobenzophenone and different aniline derivatives by both conventional and microwave methods and structures were confirmed on the basis of their TLC, IR, 1H NMR and CHN e...

The androgen receptor (AR) is an attractive target for the treatment and molecular imaging of prostate cancer. New carbon-11-labeled propanamide derivatives were first designed and synthesized as selective androgen receptor modulator (SARM) radioligands for prostate cancer imaging using the biom...

RésuméLa condensation en milieu aprotique de l'énolate de l'isopropyl phénylcétone sur le chloro-1 cyclohexène conduit à l'isopropylidène-2 cyclohexyl phénylcétone, au phényl-7 diméthyl-8,8 bicyclo-[4.2.0] octène-1ol-7 et à la diméthyl-9,9 tétrahydro-1 ,2,3,4 anthr...

Alcohol production by olefin hydration is an important reaction in the modern intermediate chemistry. The use of trifluoroacetic acid (TFA) could be a way to increase alcohol productivity by addition of the TFA to the double bond forming the corresponding ester. The product obtained by addition ...

The preparation of di-(−)-(1R,2S)-2-phenyl-1-cyclohexyl diazenedicarboxylate 4 is described. Reaction of (1R,2S)-2-phenyl-1-cyclohexanol 1 with excess phosgene in the presence of quinoline afforded chloroformate 2 which was treated directly with hydrazine monohydrate (0.5 equiv.) to afford di-(−...

Thermal decomposition of tosyl hydrazones (1) and polymer-bounded sulfonyl hydrazone (2) of cyclohexyl phenyl ketone was studied in the presence of a strong base with aprotic and protic solvent. Expected products such as benzal cyclohexane, 1-benzyl cyclohexene and 1-phenyl cycloheptene were for...

T–lymphokine-activated killer cell–originated protein kinase (TOPK) is a serine-threonine mitogen-activated protein kinase that is highly expressed in many types of human cancer. Due to its important role in cancer progression, TOPK is becoming an attractive target in chemotherapeutic drug des...

Sphingosine kinase 1 (SphK1), the enzyme that produces the bioactive sphingolipid metabolite, sphingosine-1-phosphate, is a promising new molecular target for therapeutic intervention in cancer and inflammatory diseases. In view of its importance, the main objective of this work was to find new ...

The HIV-1 capsid (CA) protein plays essential roles in both early and late stages of HIV-1 replication and is considered an important, clinically unexploited therapeutic target. As such, small drug-like molecules that inhibit this critical HIV-1 protein have become a priority for several groups....

The avicide 3‑chloro‑4‑methylanaline hydrochloride (chloro‑p‑toluidine hydrochloride, CPTH, DRC-1339) is used to control pest bird species that damage agricultural crops. A specific and sensitive gas chromatography-tandem mass spectrometry method was developed and validated for the determination...