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Unconventional Transformations of Difluorocarbene with Amines and Ethers.

ConspectusFluorine-containing compounds are extensively involved in various fields originating from intriguing and unique characteristics of … ldehydes, cascade reaction with both a nucleophile and an electrophile, or [2+1] cycloaddition with alkenes or alkynes. However, its unconventional and intriguing protocols beyond as a difluoromethyl synthon have rarely been studied, and thus, it is highly desired given its abundance, inexpensiveness and peculiar properties. In this Account, we mainly dis …

[Characteristics and Health Risk Assessment of Volatile Organic Compounds in Different Functional Zones in Baoji in Summer].

The situation of air pollution in Guanzhong Plain has been increasing in recent years; hence, it is very important to study the characterist … nt effect on aldehydes and ketones. Environmental impact assessment results revealed that OVOCs and alkenes contributed significantly to OFP and OFP from large to small was as follows:industrial zone>scenic zone>traffic zone>comprehensive zone. The range of L·OH in each functional zone was 8.77-15.82 s-1, with isoprene contributing the most in the industr …

Nitric oxide in breast cancer: induction of vascular endothelial growth factor-C and correlation with metastasis and poor prognosis.

PURPOSE: Metastasis to regional lymph nodes through the lymphatic vessels is a common step in the progression of cancer. Recent evidence suggests that tumor production of vascular endothelial growth factor-C (VEGF-C) promotes lymphagiogenesis, which in turn promotes lymphatic metastasis. Nitric oxide (NO) may also increase metastatic ability in human cancers. EXPERIMENTAL DESIGN: Nitrite/nitrate levels and VEGF-C production were assessed in MDA-MB-231 breast cancer cells after induction and/or inhibition of NO synthesis. Formation of nitrotyrosine, a biomarker for peroxynitrate formation from

Essential Medicinal Chemistry of Essential Medicines.

Since 1977, the World Health Organization publishes a list of essential medicines, i.e., those that satisfy the priority health care needs of the population and are selected with regard to disease prevalence and public health relevance, evidence of clinical efficacy, and safety, as well as comparative costs and cost-effectiveness. The Essential Medicines List (EML) is an invaluable tool for all countries to select those medicines that have an excellent risk/benefit ratio and that are reputed to be of pivotal importance to health. In the present perspective, we describe the chemical composition

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… Some toxicophorics are rare or absent 36 in the EMs, while others are recurring (e.g., alkene, alkyl halide, aniline, phenol). The presence of some structural alerts in a high percentage of EMs in part questions the need to refine the toxicophoric list, also putting the single moieties in context. … Among the two most represented structural alerts on the EML, alkenes are not overrepresented in the BBW drugs (9% compared with 13% on the EML), while alkyl halides might be (18% compared with 9%). …

Sericin-chitosan conjugated silver nanoparticles protect against 1,2-dimethylhydrazine-induced colon cancer in mice by regulating metastatic biomarkers, prohibiting dysplasia and enhancing antioxidant potential.

Colon cancer is reported as third most prevalent malignancy worldwide, while sericin being an antioxidant, is now used in biomedical applications due to its biochemical characteristics and has shown potential efficacy to treat colon cancer. Sericin was isolated by the degumming process followed by the characterization by using FTIR, UV, XRD, and SEM techniques to confirm the successful synthesis of SAgNPs and SChiAgNPs. The male Balb C mice were then divided into 13 groups. Group 1: Control, Group 2: DMH (20 mg/kg) (injected (IP) thrice a week for 14 weeks). Groups 3,4,5: Sericin (S) (100 mg/k

Angioedema and Hemorrhage After 4.5-Hour tPA (Tissue-Type Plasminogen Activator) Thrombolysis Ameliorated by T541 via Restoring Brain Microvascular Integrity.

Background and Purpose- tPA (tissue-type plasminogen activator) is the only recommended intravenous thrombolytic agent for ischemic stroke. However, its application is limited because of increased risk of hemorrhagic transformation beyond the time window. T541 is a Chinese compound medicine with potential to attenuate ischemia and reperfusion injury. This study was to explore whether T541-benefited subjects underwent tPA thrombolysis extending the time window. Methods- Male C57BL/6 N mice were subjected to carotid artery thrombosis by stimulation with 10% FeCl3 followed by 10 mg/kg tPA with/wi

Marine Natural Products as Potent Anticancer Agents (2020-2024): Structural Diversity, SARs and Target Prediction.

In recent years, Marine Natural Products (MNPs) have emerged as a significant source for anticancer drug discovery, as many natural products can offer structural diversity, unique mechanisms of action, and relatively low toxicity. This article provides a systematic review of MNPs with reported anticancer activities from 2020 to 2024. These compounds are classified into seven major categories: terpenoids, alkaloids, sterols, polyketides, peptides and proteins, polysaccharides, and macrolides. For each category, we elaborate on the marine sources, structural identification, in vitro anticancer a

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… Reduction of this group to a hydroxyl or alkene led to loss of activity, while other structural modifications also resulted in a significant decrease in potency. … Further analysis using NMR ( 1 H-NMR, 13 C-NMR) revealed that the compound has four alkenes, three carbonyls, and five unsaturation degrees, indicating a tetracyclic structure. …

Development and application of decatungstate catalyzed C-H 18F- and 19F-fluorination, fluoroalkylation and beyond.

Over the past few decades, photocatalytic C-H functionalization reactions have received increasing attention due to the often mild reaction conditions and complementary selectivities to conventional functionalization processes. Now, photocatalytic C-H functionalization is a widely employed tool, supporting activities ranging from complex molecule synthesis to late-stage structure-activity relationship studies. In this perspective, we will discuss our efforts in developing a photocatalytic decatungstate catalyzed C-H fluorination reaction as well as its practical application realized through co

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… A series of 2-methylaniliniums containing multiple C(sp 3 )–H bonds with similar properties were then selectively functionalized at the C-2 position by coupling the intermediate radical with electron-deficient alkenes (53a–53c). … In further explorations of site-selective C(sp 3 )–H functionalization, Torigoe, Kuninobu and co-workers have reported a decatungstate C(sp 3 )–H alkylation of valine derivatives 60 with electron-deficient alkenes. 100 Here, the initially alkylated product 61 undergoes hydrolysis and cyclization to afford …

Ginsenoside Rg3: Potential Molecular Targets and Therapeutic Indication in Metastatic Breast Cancer.

Breast cancer is still one of the most prevalent cancers and a leading cause of cancer death worldwide. The key challenge with cancer treatment is the choice of the best therapeutic agents with the least possible toxicities on the patient. Recently, attention has been drawn to herbal compounds, in particular ginsenosides, extracted from the root of the Ginseng plant. In various studies, significant anti-cancer properties of ginsenosides have been reported in different cancers. The mode of action of ginsenoside Rg3 (Rg3) in in vitro and in vivo breast cancer models and its value as an anti-canc

Recent Insights in Multi-Target Drugs in Pharmacology and Medicinal Chemistry.

Many of the drugs used in treatment today have been designed based on the "specificity paradigm". Resistance has developed against drugs designed using this approach, leading to a decrease in their effectiveness. In addition, it is well-documented in the literature that diseases with complex etiologies, such as Alzheimer's, Parkinson's, and cancer are influenced by multiple genetic and/or environmental factors. As a result, specificity paradigm is often insufficient for treating these diseases. Therefore, there is a need to develop drugs that interact with multiple targets simultaneously throu

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… The method offers significant adaptability and synthetic versatility, enabling the production of multitopic metal‐binding compounds with phenyl substituents and various bridging units. [ 139 ] Heck Reaction The Heck reaction facilitates the formation of substituted alkenes through the interaction of … an activated alkene and an unsaturated halide, in the presence of a palladium catalyst and a base ( Scheme 5 ). …

The role of multiparametric magnetic resonance imaging in the differentiation of low- and high-grade non-muscle invasive bladder cancer

PURPOSE: To evaluate the diagnostic efficacy of apparent diffusion coefficient (ADC) measurements and semi-quantitative dynamic contrast enhancement (DCE) parameters in predicting the differentiation between low- and high-grade tumors in non-muscle invasive bladder cancers (NMIBC). METHODS: Patients with NMIBC, who were histopathologically confirmed between August 2020 and July 2023, were analyzed by 2 radiologists with different levels of experience. DCE semi-quantitative parameters such as wash-in rate (WiR), wash-out ratio (WoR), time to peak (TTP), and peak enhancement (PE) were calculate

Piperine: From Green Extraction to Clinical Translation-A Review.

BACKGROUND: Piperine has diverse pharmacological and bioenhancing activities, but poor aqueous solubility, variable exposure, interaction liability, and discontinuity across production, formulation, and clinical evaluation limit translation. This review integrates these frequently separated stages. METHODS: A structured narrative PubMed search covered English-language studies published from 1 January 2021 to 27 April 2026, supplemented by ClinicalTrials.gov records checked through 13 June 2026, backward citation searching, and selected earlier seminal studies. Evidence was synthesized by expe

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… Image D also shares the same foundational structure, with distinct cis/trans configurations compared to A, B and C. 2D skeletal formulas of four piperine geometric isomers labeled A, B, C, D with cis and trans alkenes. … The shortened single-alkene linker in P reduced cancer-cell potency while producing a wider separation from the tested 293T cells. …

Covalent targeting of PSMD14 by Eupalinolide B induces oncoprotein degradation and apoptosis in acute promyelocytic leukemia cells.

Treatment of acute promyelocytic leukemia (APL) remains challenged by toxicities associated with current regimens, highlighting the need for novel and safer therapeutic agents. Here, we identify Eupalinolide B (EB), a natural sesquiterpene lactone isolated from Eupatorium lindleyanum DC., as a potent anti-leukemic compound targeting the human APL-derived HL-60 cell line. Through integrated chemoproteomic profiling and functional validation, we demonstrate that EB covalently binds and inhibits 26S proteasome non-ATPase regulatory subunit 14 (PSMD14), a deubiquitinase enzyme (DUB) within the 19S

Небиториальное воздействие сафронных соединений на множественный склероз: молекулярная стыковка и динамика, повышение свойств с помощью золотых наночастиц и оценка антиоксидантных, антибактериальных, цитотоксичных свойств.

Уникальные свойства наночастиц, такие, как их небольшой размер и способность пересечь мозговой барьер, делают их хорошо пригодными для целевой доставки наркотиков в центральную нервную систему. Текущие исследования направлены на разработку новаторских методов лечения наночастиц от неврологического расстройства; множественного склероза (МС). В исследовании было подтверждено, что зеленый синтез является оптимальным методом производства экологически безопасных соединений. Наночастицы характеризовались инфракрасной спектроскопией Фурье (FT-IR), диффузией рентгеновского порошка (XRD) и микроскопией

Understanding In-Person and Online Exercise Oncology Programme Delivery: A Mixed-Methods Approach to Participant Perspectives.

Alberta Cancer Exercise (ACE) is an exercise oncology programme that transitioned from in-person to online delivery during COVID-19. The purpose of this work was to understand participants' experiences in both delivery modes. Specifically, survivors' exercise facilitators and barriers, delivery mode preference, and experience with programme elements targeting behaviour change were gathered. A retrospective cohort design using explanatory sequential mixed methods was used. Briefly, 57 participants completed a survey, and 19 subsequent, optional interviews were conducted. Most participants indic

Anti-Cancer Potential of Cannabinoids, Terpenes, and Flavonoids Present in Cannabis.

In recent years, and even more since its legalization in several jurisdictions, cannabis and the endocannabinoid system have received an increasing amount of interest related to their potential exploitation in clinical settings. Cannabinoids have been suggested and shown to be effective in the treatment of various conditions. In cancer, the endocannabinoid system is altered in numerous types of tumours and can relate to cancer prognosis and disease outcome. Additionally, cannabinoids display anticancer effects in several models by suppressing the proliferation, migration and/or invasion of can

Dual COX-2/TNF-α Inhibitors as Promising Anti-inflammatory and Cancer Chemopreventive Agents: A Review.

Cyclooxygenases (COX) play a pivotal role in inflammation and are responsible for the production of prostaglandins (PGs). Two types of COXs have been identified as key biological targets for drug design: Constitutive COX-1 and inducible COX-2. Nonsteroidal anti-inflammatory drugs (NSAIDs) target COX-1, while selective COX-2 inhibitors are designed for COX-2. These COX isoforms are involved in multiple physiological and pathological pathways throughout the body. Overproduction of tumor necrosis factor-alpha (TNF-α) plays a role in COX-2's inflammatory activity. Tumor necrosis factor-alpha can c

Гут Микробиота Нарушение гематологовой терапии рака: Молекулярное понимание и последствия для эффективности лечения.

Гематологическая магнелезность (ГМ), включая лейкемию, лимфому и множественные миеломы, связана с бесконтрольным распространением аномальных кровеносных клеток, что создает серьезные клинические проблемы из-за их неоднородности и различных методов лечения. Несмотря на недавние достижения в области лечения, благодаря которым повысились показатели выживаемости, особенно в случае хронической лимфоцитической лейкемии и острой лимфоболической лейкемии, такие методы лечения, как химиотерапия и трансплантация стволовых клеток, часто нарушают микробиоту, что может негативно сказаться на результатах ле

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… Oxidoreductases reduce functional groups such as alkenes, carboxylic acids, nitrous, nitrogen oxides, azo, and sulfoxides using cofactors such as NAD(P)H, flavin, and Fe-S clusters [ 36 , 48 ]. …

Frentizole, a Nontoxic Immunosuppressive Drug, and Its Analogs Display Antitumor Activity via Tubulin Inhibition.

Antimitotic agents are one of the more successful types of anticancer drugs, but they suffer from toxicity and resistance. The application of approved drugs to new indications (i.e., drug repurposing) is a promising strategy for the development of new drugs. It relies on finding pattern similarities: drug effects to other drugs or conditions, similar toxicities, or structural similarity. Here, we recursively searched a database of approved drugs for structural similarity to several antimitotic agents binding to a specific site of tubulin, with the expectation of finding structures that could f

Homoharringtonine: updated insights into its efficacy in hematological malignancies, diverse cancers and other biomedical applications.

HHT has emerged as a notable compound in the realm of cancer treatment, particularly for hematological malignancies. Its multifaceted pharmacological properties extend beyond traditional applications, warranting an extensive review of its mechanisms and efficacy. This review aims to synthesize comprehensive insights into the efficacy of HHT in treating hematological malignancies, diverse cancers, and other biomedical applications. It focuses on elucidating the molecular mechanisms, therapeutic potential, and broader applications of HHT. A comprehensive search for peer-reviewed papers was condu