Iron–Imine Cocktail in Drug Development: A Contemporary Update DOI Open Access

Judith Anane,

Esther Owusu,

Gildardo Rivera

и другие.

International Journal of Molecular Sciences, Год журнала: 2024, Номер 25(4), С. 2263 - 2263

Опубликована: Фев. 13, 2024

Organometallic drug development is still in its early stage, but recent studies show that organometallics having iron as the central atom have possibility of becoming good candidates because an important micro-nutrient, and it compatible with many biological systems, including human body. Being eco-friendly Lewis acid, can accept lone pair electrons from imino(sp2)-nitrogen, resultant iron-imine complexes a interacting several proteins enzymes humans. Iron-imine demonstrated significant potential anticancer, bactericidal, fungicidal, other medicinal activities years. This article systematically discusses major synthetic methods pharmacological potentials vitro activity to clinical performance 2016 date. In nutshell, this manuscript offers simplistic view inorganic chemistry: for instance, presented "eco-friendly non-toxic" metal (as opposed platinum) will lead non-toxic pharmaceuticals. The abundant literature on chelators shows complexes, particularly if redox-active cells, be quite cytotoxic, which beneficial future targeted therapies. While we made every effort include all related papers, any omission purely unintentional.

Язык: Английский

Synthesis and biological evaluation of novel benzothiazole derivatives as potential anticancer and antiinflammatory agents DOI Creative Commons

Xuemei Xu,

Zhaojingtao Zhu,

Siyu Chen

и другие.

Frontiers in Chemistry, Год журнала: 2024, Номер 12

Опубликована: Март 18, 2024

Introduction: Cancer, a significant global health concern, necessitates innovative treatments. The pivotal role of chronic inflammation in cancer development underscores the urgency for novel therapeutic strategies. Benzothiazole derivatives exhibit promise due to their distinctive structures and broad spectrum biological effects. This study aims explore new anti-tumor small molecule drugs that simultaneously anti-inflammatory anticancer based on advantages benzothiazole frameworks. Methods: compounds were characterized by nuclear magnetic resonance (NMR), liquid chromatograph-mass spectrometer (LC-MS) high performance chromatography (HPLC) structure as well purity other related physicochemical properties. effects proliferation human epidermoid carcinoma cell line (A431) non-small lung lines (A549, H1299) evaluated MTT method. effect expression levels inflammatory factors IL-6 TNF-α mouse monocyte macrophages (RAW264.7) was assessed using enzyme-linked immunosorbent assay (ELISA). apoptosis cycle A431 A549 cells flow cytometry. migration scratch wound healing assay. protein Western Blot parameters, pharmacokinetic properties, toxicity drug similarity active compound predicted Swiss ADME admetSAR web servers. Results: Twenty-five designed synthesized, with confirmed through spectrogram verification. 6-chloro- N -(4-nitrobenzyl) benzo[d] thiazol-2-amine (compound B7 ) screened series bioactivity assessments, which significantly inhibited A431, H1299 cells, decreased activity TNF-α, hindered migration. In addition, at concentrations 1, 2, 4 μM, exhibited apoptosis-promoting cycle-arresting similar those lead 7-chloro- -(2, 6-dichlorophenyl) thiazole-2-amine 4i ). blot analysis both AKT ERK signaling pathways cells. prediction results ADMET indicated had good Discussion: has innovatively developed derivatives, focus its notable dual activities. stands out ability reduce A549, lower cytokines TNF-α. These position promising candidate dual-action therapy. study’s mechanistic exploration, highlighting ’s simultaneous inhibition pathways, offers strategy addressing survival mechanisms tumor milieu facilitating progression.

Язык: Английский

Процитировано

8

A Concise Review on Recent Development of Indole Derivatives for Anticancer Activities DOI

B. T. Sridhar,

Nagesh Gunavanthrao Yernale,

Ramesh S. Gani

и другие.

Journal of the Indian Chemical Society, Год журнала: 2024, Номер 101(10), С. 101282 - 101282

Опубликована: Июль 24, 2024

Язык: Английский

Процитировано

6

Exploring magnetically recoverable catalysts for the synthesis of benzoxazoles derivatives DOI Creative Commons

Fadhel F. Sead,

Jayanti Makasana,

Shelesh krishna saraswat

и другие.

Applied Catalysis O Open, Год журнала: 2025, Номер unknown, С. 207031 - 207031

Опубликована: Фев. 1, 2025

Язык: Английский

Процитировано

0

Benzimidazole(s): synthons, bioactive lead structures, total synthesis, and the profiling of major bioactive categories DOI Creative Commons
Lotfi M. Aroua, Fahad M. Alminderej, Hind R. Almuhaylan

и другие.

RSC Advances, Год журнала: 2025, Номер 15(10), С. 7571 - 7608

Опубликована: Янв. 1, 2025

Benzimidazole, a fused bicyclic compound with benzene and pentacyclic 1,3-diazole moeities, has simple aromatic heterocyclic structure. The moiety become an indispensable anchor for the development of new pharmacologically active products, yielded several therapeutic agents anticancer, antihypertensive, antimicrobial, antifungal antiulcer effects. Benzimidazoles, as synthetically feasible pharmacophoric synthons, have been relentlessly pursued preparation analogues derivatives, they successfully developed into some most sought-after vital pharmacophores drug discovery. use varied substituents differing patterns around benzimidazole nucleus provided wide spectrum biological activities. In addition, constitutes building block production drugs, candidates, chemical entities, lead molecules. importance this bioactivity, e.g., antibacterial, antitubercular, antidiabetic, antifungal, anti-inflammatory, analgesic, antioxidant, antihistaminic, antimalarial activity, led us to take note provide overview synthetic approaches various derivatives together their actions. This review is projected further assist in design benzimidazole-based compounds optimized products towards drug-development strategies.

Язык: Английский

Процитировано

0

Copper Methacrylate Complexes with Benzimidazole Derivatives: Structural Characterization and Antimicrobial Assays DOI Creative Commons

Andra-Georgeta Andrei,

Rodica Olar, Cătălin Maxim

и другие.

Inorganics, Год журнала: 2025, Номер 13(4), С. 109 - 109

Опубликована: Апрель 1, 2025

In order to design antimicrobial species, a series of methacrylate (Macr) complexes, [Cu(HBzIm)2(Macr)2] (1), [Cu2(HBzIm)2(Macr)4] (2), [Cu(2-MeBzIm)2(Macr)2] (3), [Cu2(2-MeBzIm)2(Macr)4] (4), and [Cu(5,6-Me2BzIm)2(Macr)2] (5) (HBzIm = benzimidazole, 2-MeBzIm 2-methylbenzimidazole, 5,6-Me2BzIm 5,6-dimethylbenzimidazole) were synthesized characterized by several spectral techniques, as well single crystal X-ray diffraction. The mononuclear species exhibit distorted octahedral stereochemistry, while the binuclear types, with paddle-wheel structure, adopt square pyramidal surrounding. acts either chelate or bridge, all benzimidazole derivatives are coordinated unidentate. supramolecular networks developed both intermolecular π–π stacking interactions hydrogen bonds. assays provided complexes ability inhibit planktonic strain proliferation, adhere on inert substratum. All moderate activity, in regards standard clinical isolate strains, most active being compound 5 against Candida albicans, minimum inhibitory concentration (MIC) 0.156 mg/mL. It is worth mentioning that complex 1 inhibited microbial adhesion Escherichia coli 2 constrained C. albicans strain.

Язык: Английский

Процитировано

0

The Amyloid Beta Aggregation Inhibition Properties of New Pt (II) Complexes and Their Potential in Alzheimer's Treatment DOI Creative Commons
Salih Günnaz, Onur Şahın, S. İrişli

и другие.

Applied Organometallic Chemistry, Год журнала: 2025, Номер 39(5)

Опубликована: Апрель 10, 2025

ABSTRACT In this study, N‐phenylortho‐phenylenediamine and N‐phenyl ethylenediamine were utilized as amines, two novel ligands, benzimidazole (LI) Schiff base (LII), synthesized through condensation reactions with 3‐methoxy‐4‐benzyloxybenzaldehyde. Furthermore, using these same LIII (benzimidazole) 3‐phenoxybenzaldehyde LIV (Schiff base) 4‐benzyloxybenzaldehyde in accordance the literature. Then, Pt (II) complexes (Ia, Ib, II, III, IV) prepared it was determined that Ia Ib are geometric isomers. The ligands characterized 1 H‐NMR, 13 C‐NMR, FT‐IR, elemental analysis methods. cytotoxic effects of evaluated on SH‐SY5Y neuronal cells. Low‐toxicity Ia, IV then tested for their ability to inhibit amyloid beta (Aβ 1–42 ) aggregation. Thioflavin T fluorescence analysis, AFM imaging, MALDI‐TOF mass spectrometry demonstrated complexes, particularly at a 1:1 complex‐to‐amyloid molar ratio, effectively inhibited Aβ These findings suggest containing may be effective against Alzheimer's disease by alleviating toxicity.

Язык: Английский

Процитировано

0

Synthesis, Anti-Inflammatory Activity, Inverse Molecular Docking, and Acid Dissociation Constants of New Naphthoquinone-Thiazole Hybrids DOI
Çağla Efeoğlu,

Sena Taskin,

Özge Selcuk

и другие.

Bioorganic & Medicinal Chemistry, Год журнала: 2023, Номер 95, С. 117510 - 117510

Опубликована: Ноя. 1, 2023

Язык: Английский

Процитировано

12

Indole-Containing Metal Complexes and Their Medicinal Applications DOI Creative Commons
Zahra Kazemi, Hadi Amiri Rudbari, Nakisa Moini

и другие.

Molecules, Год журнала: 2024, Номер 29(2), С. 484 - 484

Опубликована: Янв. 18, 2024

Indole is an important element of many natural and synthetic molecules with significant biological activity. Nonetheless, the co-presence transitional metals in organic scaffold may represent factor development effective medicinal agents. This review covers some latest most relevant achievements pharmacological activity indole-containing metal complexes area drug discovery.

Язык: Английский

Процитировано

4

Recent Advances in the Fixation of CO2 into Quinazoline and Benzimidazole DOI

Dhanusha Rajanna,

Puneethkumar M. Srinivasappa,

Allwin Sudhakaran

и другие.

Energy & Fuels, Год журнала: 2024, Номер 38(10), С. 8481 - 8515

Опубликована: Апрель 24, 2024

CO2 is an important component of the atmosphere that helps in balancing Earth's atmospheric temperature and channelizes food cycles. However, increase or decrease concentration will severely affect climate. Particularly, rise levels has immensely contributed to global warming, resulting elevated temperature, altered precipitation patterns, glacier melting, subsequent rises sea levels, impacting human well-being. In response, researchers are exploring strategies capture convert into valuable products, such as methanol, formic acid, organic compounds. synthesis compounds using CO2, like benzimidazole quinazolines, a high impact. Benzimidazole, widely used medicinal chemistry for treating cancer stomach ulcers, also exhibits antiviral antifungal properties. Quinazoline derivatives, essential drugs prazosin doxazosin, have applications post-traumatic stress disorder Alzheimer's disease. These were synthesized mainly environmentally harmful synthons phosgene potassium cyanide. To address both environmental health concerns, delving chemical fixation sustainable green production. Catalysis emerges key principle chemistry, with catalysts reducing activation energy facilitating processes. This review discusses recent state art on development various conversion quinazoline benzimidazole, through homogeneous heterogeneous catalysts. Notably, while lack industrial recyclability, show promise large-scale implementation. comprehensive mechanistic aspects DFT studies understanding better. Toward end, it gives future scope this subject.

Язык: Английский

Процитировано

4

Apoptotic cell death of stomach cancer lines (AGS) induced by Co-NTB complex through cellular organelles and DNA damage DOI Creative Commons

Sri Renukadevi Balusamy,

Mani Balamurugan,

Sumitha Purushothaman

и другие.

RSC Advances, Год журнала: 2025, Номер 15(2), С. 739 - 747

Опубликована: Янв. 1, 2025

Given that stomach cancer is the fourth leading cause of cancer-related death, there a need to develop new drugs. Among various methods, metal-based coordination compounds are considered as an efficient strategy against this type cancer. Similarly, benzimidazole moiety plays crucial role in biology; thus, benzimidazole-based have been found be active potential anticancer drugs and currently used clinical trials. In study, we explored cobalt(ii) complex agent AGS cell lines. Interestingly, MTT assay Co-NTB shows lower IC

Язык: Английский

Процитировано

0