Many researchers around the world are working on development of novel anticancer drugs with different mechanisms action. In this case, coumarin is a highly promising pharmacophore for drugs. Besides, hybridization moiety other pharmacophores has emerged as potent breakthrough in treatment cancer to decrease its side effects and increase efficiency. This review aims provide comprehensive overview recent derivatives their application Herein, we highlight describe largest number research works...

Spiro heterocycle frameworks are a class of organic compounds that possesses unique structural features making them highly sought-after targets in drug discovery due to their diverse biological and pharmacological activities.

Abstract In terms of pharmaceuticals and biological applications, synthesis complex organic molecules is a significant fast‐developing area. this context, electrosynthesis an alternative way to the traditional methods for chemo‐, regio‐, stereoselective syntheses. Electro‐organic reactions occur at room temperature normal pressure, through transferring electrons. It has been found that mild approach preparing electrophilic substrates, bases, nucleophiles in situ , from highly stable...

A molecularly defined copper acetylide cluster with ancillary N-heterocyclic carbene (NHC) ligands was prepared under acidic reaction conditions. This is the first molecular complex that features high activity in copper-catalyzed azide-alkyne cycloadditions (CuAAC) added acetic acid even at -5 °C. Ethyl propiolate protonates acetate of dinuclear precursor to release and replaces one out four ligands. Two copper(I) ions are thereby liberated form core a yellow dicationic C2-symmetric hexa-NHC...

Abstract The unique reactivity and beneficial features of the 5-aminotetrazole synthon (1H-tetrazol-5-amine) have made it a versatile effective building block in synthesis heterocyclic compounds. In addition, several drugs containing this scaffold with wide array biological properties been already introduced. Heterocyclic structures are backbone many biologically active industrially important 5-Aminotetrazole is one favored synthons used preparation heterocycle-bearing compounds, especially...

An efficient multicomponent reaction of newly designed β-trifluoromethyl β-diazo esters, acetonitrile, and carboxylic acids via an interrupted esterification process under copper-catalyzed conditions has been developed, which affords various unsymmetrical N , -diacyl-β-amino esters in good to excellent yields. The features mild conditions, a wide scope β-amino acids, also applicability large-scale synthesis, thus providing way for the synthesis β-diacylamino esters. Furthermore, this...

Abstract Herein, we have synthesized a microspherical nickel‐cobalt‐layered double hydroxides‐reduced graphene oxide composite (NiCo‐LDHs‐rGO) through one‐step hydrothermal method and then used it as an adsorbent for the removal of Pb 2+ from aqueous solutions. Fourier transform infrared spectrophotometry (FT‐IR), field emission scanning electron microscopy (FESEM), mapping elemental analysis, dispersive x‐ray spectroscopy (EDX), diffraction analysis (XRD), Brunauer–Emmett–Teller (BET) were...

A novel electrochemical iodination/spirocyclization reaction of 3-alkynyl indoles with n-Bu4NI as coupling partner and electrolyte is developed, which affords iodovinyl spiroindolenine-cyclopentanes products in excellent yields high E-stereoselectivities. This...

Site-selective bioconjugation of cysteine-containing peptides and proteins is currently achieved via a maleimide–thiol reaction (Michael addition). When maleimide-functionalized chelators are used the resulting bioconjugates subsequently radiolabeled, instability has been observed both during radiosynthesis post-injection in vivo, reducing radiochemical yield negatively impacting performance. Recently, phenyloxadiazolyl methylsulfone derivative (PODS) was proposed as an alternative to...

Radiometal-based radiopharmaceuticals bearing bifunctional HBED chelators are powerful radiotracers for cancer diagnosis and therapy. Bifunctional make strong complexes with trivalent gallium able to bind bioactive molecules through covalent bonds. However, thus far, no chelator capable of direct conjugation via click chemistry has been reported. We hereby introduce HBED-NN as a structurally new coupling. also investigated the complex [Ga-(HBED-NN)] potential use in gallium-based...

A dinuclear N -heterocyclic carbene (NHC) copper complex efficiently catalyzes azide–alkyne cycloaddition (CuAAC) “click” reactions. The ancillary ligand comprises two 4,5-dimethyl-1,3-thiazol-2-ylidene units and an ethylene linker. three-step preparation of the from commercially available starting compounds is more straightforward cost-efficient than that previously described 1,2,4-triazol-5-ylidene derivatives. Kinetic experiments revealed its high catalytic CuAAC activity in organic...

In radiopharmaceutical syntheses, maleimide is commonly used for linking thiol-bearing bioactive molecules to metal–complexing ligands (chelators).

In this work, the coordination sphere of a newly synthesized aluminum HBED cage has been investigated by using 2D NMR and DFT calculations.

HBED-CC is a bifunctional complexing agent that, at ambient temperature, tightly chelates the trivalent radiometal 68Ga (T1/2 = 68 min). This has attracted lot of interest in tumor imaging applications. Depending on chemical structure, different variants may be employed as radiolabeling precursor for synthesis desired radiopharmaceuticals. In this context, HBED-CC-tris(tert-butyl ester) only known monovalent variant which used non-symmetric HBED-CC-based Commercial very ­expensive, with...

Abstract Ein molekular definierter Kupferacetylidcluster mit N‐heterocyclischen Carben‐Steuerliganden (NHC) wurde zum ersten Mal unter sauren Reaktionsbedingungen hergestellt. Dieser Cluster ist der erste molekulare Kupferacetylid‐Komplex, eine hohe Aktivität in Kupfer‐katalysierten Azid‐Alkin‐Cycloaddition aufweist, bei Essigsäurezusatz sogar −5 °C. Ethylpropiolat protoniert alle Acetatliganden des zweikernigen Vorläuferkomplexes zu Essigsäure und ersetzt jeden vierten Steuerliganden. Als...

Hydroxanthones have attracted considerable attention due to their significance in organic and biological chemistry, yet synthesis remains a great challenge. In this study, series of chromone-tethered alkenes are designed, radical cyclization reaction these chromone derivatives has been achieved under photoredox conditions. The uses bromodifluoroacetamides or bromodifluoroacetates as coupling partners, affording broad range functionalized tetrahydroxanthone products with up 85% yields. is...

Protection of carbonyl compounds with 1,3-propanedithiol under a catalyst-free condition in nitromethane as solvent has been described.

Bifunctional HBED chelators are hexadentate complexing ligands (chelators) that tightly coordinate to trivalent gallium and, additionally, able bind bioactive molecules. In nuclear medicine, HBED-based radiopharmaceuticals used as powerful radiotracers for tumor imaging. Among variants of bifunctional chelators, HBED-CC is the most well-known; it possesses two terminal carboxylic acid groups undergo bioconjugation by amide-bond formation. However, permit through click coupling, we previously...

Au(I)-catalyzed reactions have emerged as an important tool for various organic transformations in the past decade, especially cross-coupling reactions. However, exceptionally high reduction potential value of Au(I)|Au(III) redox couple may act obstacle its development. using external mild oxidants gold-catalyzed solves this problem effectively. This review gives overview different types employed Such function via two general mechanistic pathways which either oxidation state Au(I) atom...