Synthesis of alkyl sulfones a photocatalytic multicomponent reaction of aryldiazo tetrafluoroborate salts, styrene derivatives, and sodium metabisulfite.

Alkyl sulfones are found in numerous valuable organic molecules. Here, we describe a promising approach for the one-pot synthesis of alkyl sulfones under visible light. Aryl diazo salts were allowed to react with styrene derivatives and sodium metabisulfite in the presence of thiophenol as a hydrogen atom transfer reagent and rhodamine B as a photocatalyst to yield alkyl sulfones.

Recent Progress in Synthesis of Tc-labeled Complexes with Nitroimidazoles as SPECT Probes for Targeting Tumor Hypoxia.

The majority of solid tumors have hypoxia, or low oxygen levels, which is one of the hallmarks of cancer. Hypoxia was found to relate to cancer metastases and resistance to therapies, therefore, detection of hypoxia plays an important role in the process of cancer prognosis and treatment. Single-photon emission computed tomography (SPECT) is a non-invasive imaging technique using gamma-emitting radiopharmaceuticals to visualize biological activities within the body.

Visible-light-mediated synthesis of oxime esters multicomponent reactions of aldehydes, aryl amines, and -hydroxyphthalimide esters.

Oxime esters are useful scaffolds in many organic chemistry transformations. Herein, a novel visible-light-mediated three-component reaction for synthesis of oxime esters is reported. Aldehydes, aniline, and -hydroxyphthalimide (NHPI) esters were used as substrates in this three-component reaction, and eosin Y was used as a crucial photocatalyst for the reaction.

Direct transformation of benzyl esters into esters, amides, and anhydrides using catalytic ferric(III) chloride under mild conditions.

A facile one-pot transformation of benzyl esters into esters, amides, and anhydrides is described. α,α-Dichlorodiphenylmethane and FeCl were employed as the chlorinating agent and catalyst respectively to convert benzyl esters into acid chloride intermediates, which directly reacted with alcohols, amines, and carboxylic acids. Various esters, amides, and anhydrides were readily obtained with high yields under mild conditions.

Evaluation of novel pyrazol-4-yl pyridine derivatives possessing arylsulfonamide tethers as c-Jun N-terminal kinase (JNK) inhibitors in leukemia cells.

A series of 36 pyrazol-4-yl pyridine derivatives (8a-i, 9a-i, 10a-i, and 11a-i) was designed, synthesized, and evaluated for its antiproliferative activity over NCI-60 cancer cell line panel and inhibitory effect against JNK isoforms (JNK1, JNK2, and JNK3). All the synthesized compounds were tested against the NCI-60 cancer cell line panel. Compounds 11b, 11c, 11g, and 11i were selected to determine their GI and exerted a superior potency over the reference standard SP600125 against the tested cell lines.

Tin(II) Chloride-Catalyzed Direct Esterification and Amidation of -Butyl Esters Using α,α-Dichlorodiphenylmethane Under Mild Conditions.

A practical one-pot synthesis of esters and amides from -butyl esters acid chloride was developed. Reactions of -butyl esters with α,α-dichlorodiphenylmethane as the chlorinating agent and SnCl as catalyst-generated acid chloride intermediates were subsequently used in reactions with a variety of alcohols and amines to afford the corresponding esters and amides in high yields under mild reaction conditions. This catalytic synthetic procedure offers an effective strategy for the facile esterification and amidation of -butyl esters.

Recent Developments in PET and SPECT Radiotracers as Radiopharmaceuticals for Hypoxia Tumors.

Hypoxia, a deficiency in the levels of oxygen, is a common feature of most solid tumors and induces many characteristics of cancer. Hypoxia is associated with metastases and strong resistance to radio- and chemotherapy, and can decrease the accuracy of cancer prognosis. Non-invasive imaging methods such as positron emission tomography (PET) and single-photon emission computed tomography (SPECT) using hypoxia-targeting radiopharmaceuticals have been used for the detection and therapy of tumor hypoxia.

Recent Advances of Ga-Labeled PET Radiotracers with Nitroimidazole in the Diagnosis of Hypoxia Tumors.

Positron emission tomography (PET) is a noninvasive molecular imaging method extensively applied in the detection and treatment of various diseases. Hypoxia is a common phenomenon found in most solid tumors. Nitroimidazole is a group of bioreducible pharmacophores that selectively accumulate in hypoxic regions of the body.

Visible-light-driven reactions for the synthesis of sulfur dioxide-inserted compounds: generation of S-F, S-O, and S-N bonds.

Sulfur dioxide-containing compounds such as sulfonyl fluorides, sulfonyl esters, and sulfonyl amides are important structural frameworks in many natural products, pharmaceuticals, and organic compounds. Thus, synthesis of these molecules is a very valuable research topic in organic chemistry. Various synthetic methods to introduce SO groups into the structure of organic compounds have been developed for the synthesis of biologically and pharmaceutically useful compounds.

Recent Advances in Synthetic Routes to Azacycles.

A heterocycle is an important structural scaffold of many organic compounds found in pharmaceuticals, materials, agrochemicals, and biological processes. Azacycles are one of the most common motifs of a heterocycle and have a variety of applications, including in pharmaceuticals. Therefore, azacycles have received significant attention from scientists and a variety of methods of synthesizing azacycles have been developed because their efficient synthesis plays a vital role in the production of many useful compounds.

F-Radiolabeled Translocator Protein (TSPO) PET Tracers: Recent Development of TSPO Radioligands and Their Application to PET Study.

Translocator protein 18 kDa (TSPO) is a transmembrane protein in the mitochondrial membrane, which has been identified as a peripheral benzodiazepine receptor. TSPO is generally present at high concentrations in steroid-producing cells and plays an important role in steroid synthesis, apoptosis, and cell proliferation. In the central nervous system, TSPO expression is relatively modest under normal physiological circumstances.

Visible-light-driven SAQS-catalyzed aerobic oxidative dehydrogenation of alkyl 2-phenylhydrazinecarboxylates.

Azo compounds are useful molecules with a wide range of applications in organic chemistry. Here, a novel visible-light-driven oxidative dehydrogenation of alkyl 2-phenylhydrazinecarboxylates is used for the synthesis of azo compounds. This synthetic method was conducted under an aerobic environment with mild reaction conditions.

Visible-light-induced one-pot synthesis of sulfonic esters multicomponent reaction of arylazo sulfones and alcohols.

Sulfonic ester is a chemical structure common to many organic molecules, including biologically active compounds. Herein, a visible-light-induced synthetic method to prepare aryl sulfonic ester from arylazo sulfones was developed. In the present study, a one-pot reaction was carried out using arylazo sulfones, DABSO (DABCO·(SO)), and alcohols in the presence of CuI as a coupling catalyst and HCl as an additive to yield sulfonic esters multicomponent reaction.

Practical one-pot amidation of -Alloc-, -Boc-, and -Cbz protected amines under mild conditions.

A facile one-pot synthesis of amides from -Alloc-, -Boc-, and -Cbz-protected amines has been described. The reactions involve the use of isocyanate intermediates, which are generated in the presence of 2-chloropyridine and trifluoromethanesulfonyl anhydride, to react with Grignard reagents to produce the corresponding amides. Using this reaction protocol, a variety of -Alloc-, -Boc-, and -Cbz-protected aliphatic amines and aryl amines were efficiently converted to amides with high yields.

Facile tin(II)-catalyzed synthesis of -heterocycles from dicarboxylic acids and arylamines.

A novel efficient transformation reaction of dicarboxylic acids into -aryl-substituted azacycles is described. In this synthetic procedure, both catalytic SnCl and phenylsilane were used as crucial reagents for reaction of arylamines with dicarboxylic acids to produce the desired azacycles. Using this SnCl-catalyzed synthetic method, various -aryl-substituted azacycles were successfully prepared from arylamines with dicarboxylic acids in high yield.

Structural optimization of 4-(imidazol-5-yl)pyridine derivatives affords broad-spectrum anticancer agents with selective B-RAF/p38α kinase inhibitory activity: Synthesis, in vitro assays and in silico study.

In the current article, we introduce design of a new series of 4-(imidazol-5-yl)pyridines with improved anticancer activity and selective B-RAF/p38α kinase inhibitory activity. Based on a previous work, a group of structural modifications were applied affording the new potential antiproliferative agents. Towards extensive biological assessment of the target compounds, an in vitro anticancer assay was conducted over NCI 60-cancer cell lines panel representing blood, lung, colon, CNS, skin, ovary, renal, prostate, and breast cancers.

Visible-Light-Induced Catalytic Selective Halogenation with Photocatalyst.

Halide moieties are essential structures of compounds in organic chemistry due to their popularity and wide applications in many fields such as natural compounds, agrochemicals, and pharmaceuticals. Thus, many methods have been developed to introduce halides into various organic molecules. Recently, visible-light-driven reactions have emerged as useful methods of organic synthesis.

Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE Productions and Nitric Oxide in Murine RAW 264.7 Macrophages.

A series of thirteen triarylpyrazole analogs were investigated as inhibitors of lipopolysaccharide (LPS)-induced prostaglandin E (PGE) and nitric oxide (NO) production in RAW 264.7 macrophages. The target compounds - have first been assessed for cytotoxicity against RAW 264.

The HDAC1 Inhibitor CBUD-1001 Enhances TRAIL-induced Apoptosis in Colorectal Cancer Cells.

Background/aim: Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a potential anti-tumor agent. However, resistance to TRAIL has been reported in a number of clinical trials. In this study, we investigated the molecular mechanisms by which a novel histone deacetylase (HDAC) inhibitor, CBUD-1001, sensitizes colorectal cancer (CRC) cells to TRAIL-induced apoptosis.

Recent Advances in Photo-mediated Radiofluorination.

Carbon-fluorine bond formations have received a lot of attention because organofluorine compounds are widely used in pharmaceutical, agricultural, and materials science applications. In particular, the incorporation of fluorine-18, which is a commonly used radioisotope for radiopharmaceuticals for positron emission tomography (PET), a molecular imaging tool for the visualization of biochemical events, human metabolism processes, and the measurement and diagnosis of diseases in humans, plays a crucial role in clinical and preclinical studies. Several synthetic methodologies for carbon-fluorine-18 bond formation have been developed.

Synthesis and evaluation of multivalent nitroimidazole-based near-infrared fluorescent agents for neuroblastoma and colon cancer imaging.

Hypoxia is one of key characteristics of microenvironments of solid tumors, and evaluation of hypoxia status in solid tumors is important to determine cancer stage and appropriate treatment. In the present study, novel, multivalent, near-infrared (NIR) fluorescent imaging agents were developed to measure tumor hypoxia. These agents were synthesized using an amino acid as a backbone to connect mono-, bis-, or tris-2-nitroimidazole as a hypoxia-sensitive moiety to enhance uptake by the tumor and to attach sulfo-Cyanine 5.

Genome-Wide Association Study Identifies Eight Novel Loci for Susceptibility of Scrub Typhus and Highlights Immune-Related Signaling Pathways in Its Pathogenesis.

Scrub typhus is a fatal zoonotic disease caused by . This disease is accompanied by systemic vasculitis, lymphadenopathy, headache, myalgia, and eschar. In recent studies, a novel strain that is resistant to current medical treatment was identified in Thailand.

Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF/p38α inhibitors.

The synergistic effect of dual inhibition of serine/threonine protein kinases that are involved in the same signalling pathway of the diseases can exert superior biological benefits for treatment of these diseases. In the present work, a new series of (imidazol-5-yl)pyrimidine was designed and synthesized as dual inhibitors of BRAF and p38α kinases which are considered as key regulators in mitogen-activated protein kinase (MAPK) signalling pathway. The target compounds were evaluated for dual kinase inhibitory activity.

Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38α/MAPK14 inhibitor.

P38α/MAPK14 is intracellular signalling regulator involved in biosynthesis of inflammatory mediator cytokines (TNF-α, IL-1, IL-6, and IL-1b), which induce the production of inflammatory proteins (iNOS, NF-kB, and COX-2). In this study, drug repurposing strategies were followed to repositioning of a series of B-RAF imidazol-5-yl pyridine inhibitors to inhibit P38α kinase. A group 25 reported P38α kinase inhibitors were used to build a pharmacophore model for mapping the target compounds and proving their affinity for binding in P38α active site.

F-labelled BODIPY dye as a dual imaging agent: Radiofluorination and applications in PET and optical imaging.

Dual Positron emission tomography (PET)/optical imaging techniques have captured scientific interest for clinical applications due to their potential as an effective tool for visualizing in vivo information such as disease processes. 4,4'-Difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) dye has been considered an ideal platform strategy to achieve dual PET/optical imaging due to its photochemical nature and chemical structure. Various radiofluorination methods to prepare [F]BODIPY dye have been developed and established, ranging from nucleophilic substitution reactions to isotope exchange reactions.