ChemMedChem最新文献_第2页

Design, Synthesis, and Biological Evaluation of Novel Triazine-Based Dual Histone Deacetylase/phosphatidylinositol 3-kinase Inhibitors for Breast Cancer Therapy. 新型三嗪类双组蛋白去乙酰化酶/磷脂酰肌醇3-激酶抑制剂用于乳腺癌治疗的设计、合成和生物学评价

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-28 DOI: 10.1002/cmdc.202501041

Lara Luzietti, Gustavo Salgado Pires, Ana Ryan, Crisamie Regidor, Matthew Hiller, Danilo Sarti, Tríona Ní Chonghaile, Pedro de Sena Murteira Pinheiro, Damir Varešlija, Daniel Alencar Rodrigues

{"title":"Design, Synthesis, and Biological Evaluation of Novel Triazine-Based Dual Histone Deacetylase/phosphatidylinositol 3-kinase Inhibitors for Breast Cancer Therapy.","authors":"Lara Luzietti, Gustavo Salgado Pires, Ana Ryan, Crisamie Regidor, Matthew Hiller, Danilo Sarti, Tríona Ní Chonghaile, Pedro de Sena Murteira Pinheiro, Damir Varešlija, Daniel Alencar Rodrigues","doi":"10.1002/cmdc.202501041","DOIUrl":"https://doi.org/10.1002/cmdc.202501041","url":null,"abstract":"Breast cancer is the most frequently diagnosed malignancy and a leading cause of cancer-related mortality among women worldwide. Triple-negative breast cancer (TNBC) poses a major clinical challenge due to its aggressive nature, limited therapeutic options, and high propensity for drug resistance. Dysregulation of the phosphatidylinositol 3-kinase (PI3K)/AKT/mTOR and histone deacetylase (HDAC) signaling pathways has been implicated in TNBC progression and therapeutic resistance, highlighting their potential as combinatorial targets. In this study, we report the design, synthesis, and biological evaluation of a novel series of triazine-based multitarget inhibitors aimed at the dual inhibition of PI3K and HDAC. Among the synthesized compounds, 5b and 5f demonstrated the most promising profiles, exhibiting low nanomolar IC50 values against HDAC6 (2.33 and 6.02 nM) and PI3Kα (17.5 and 236 nM), respectively. Both compounds reduced cell viability in breast cancer cell lines, with IC50 values below 5 µM in MDA-MB-231 cells. Western blot analysis confirmed inhibition of HDAC and PI3K signaling in treated cells. Molecular docking and dynamics simulations further revealed stable binding modes and favorable interactions within the active sites of both targets. Overall, 5b and 5f represent promising lead candidates for further optimization toward the development of novel dual HDAC/PI3K inhibitors with potential application in TNBC therapy, as evaluated in TNBC-relevant models.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 8","pages":"e202501041"},"PeriodicalIF":3.4,"publicationDate":"2026-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13110364/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147758180","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Antiproliferative Activity and Acute Toxicity of α,β-Bis(diphenylphosphine Oxide)ethanes Obtained by Bisphosphorylation of Acetylenes: Electrosynthesis Under Mild Conditions Versus Improved Superbasic Medium Synthesis. 乙炔双磷酸化制备的α，β-双（二苯基氧化膦）乙烷的抗增殖活性和急性毒性：温和条件下的电合成与改进的超碱性介质合成。

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-28 DOI: 10.1002/cmdc.70285

Maxim V Tarasov, Tatyana V Gryaznova, Kamil Ivshin, Sergey A Katsyuba, Oksana A Lenina, Anna P Lyubina, Andrey A Parfenov, A D Voloshina, Yulia H Budnikova

{"title":"Antiproliferative Activity and Acute Toxicity of α,β-Bis(diphenylphosphine Oxide)ethanes Obtained by Bisphosphorylation of Acetylenes: Electrosynthesis Under Mild Conditions Versus Improved Superbasic Medium Synthesis.","authors":"Maxim V Tarasov, Tatyana V Gryaznova, Kamil Ivshin, Sergey A Katsyuba, Oksana A Lenina, Anna P Lyubina, Andrey A Parfenov, A D Voloshina, Yulia H Budnikova","doi":"10.1002/cmdc.70285","DOIUrl":"https://doi.org/10.1002/cmdc.70285","url":null,"abstract":"A series of vicinal bis(diphenylphosphine oxide)ethanes were synthesized via the α,β-bisphosphorylation of aryl-substituted acetylenes. Optimized reaction conditions were established, affording the desired compounds in moderate to good yields. The synthesized derivatives were evaluated for cytotoxic activity against a panel of cancer cell lines (M-HeLa, MCF-7, HuTu 80, A549), and nonmalignant cells (WI-38 and Chang Liver). The highest efficacy was observed against the M-HeLa cell line, with IC50 values ranging from 1.4 to 3.9 μM, which is 9-25 times more potent than the activity of sorafenib, a reference drug. Lead compounds 3g and 3d demonstrated selectivity toward M-HeLa cells compared to Chang liver cells, suggesting their potential therapeutic value. Mechanistic investigations revealed that 3g and 3d induce dose-dependent apoptosis via the mitochondrial pathway. Key findings indicate G2/M phase cell cycle arrest independent of the p53 pathway. Furthermore, a significant decrease in tubulin polymerization-promoting protein (TPPP) levels was observed, indicating tubulin depolymerization and antimitotic activity. Additionally, compound 3d exhibited inhibitory activity against cyclin-dependent kinase 2 (CDK2). These results position bis(diphenylphosphine oxide) derivatives as a promising scaffold for the development of novel anticancer agents.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 8","pages":"e70285"},"PeriodicalIF":3.4,"publicationDate":"2026-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147758197","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synergy of Bacterial Lipid Liposomes and Monoterpene-Mediated Membrane Perturbation for Enhanced Intracellular Mycobacteria Eradication and Biofilm Disruption. 细菌脂质脂质体和单萜烯介导的膜扰动对增强细胞内分枝杆菌根除和生物膜破坏的协同作用。

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-28 DOI: 10.1002/cmdc.202501110

Nishant Pandey, Kaustav Mondal, Shivam Sharma, Debanya Pradhan, Shobhna Kapoor

{"title":"Synergy of Bacterial Lipid Liposomes and Monoterpene-Mediated Membrane Perturbation for Enhanced Intracellular Mycobacteria Eradication and Biofilm Disruption.","authors":"Nishant Pandey, Kaustav Mondal, Shivam Sharma, Debanya Pradhan, Shobhna Kapoor","doi":"10.1002/cmdc.202501110","DOIUrl":"https://doi.org/10.1002/cmdc.202501110","url":null,"abstract":"In this work, we created liposomes using lipids from the outer membrane layer of Mycobacterial smegmatis (Msm) and doped them with rifampicin and lipophilic terpene, limonene, resulting in a dual-loaded liposomal formulation. Limonene incorporation resulted in a prolonged release of encapsulated rifampicin over time and reduced minimum inhibitory concentration in comparison to the free drug or limonene-free liposomes loaded solely with the drug. Limonene showed a prolonged release over several days and could potentially find applications in fragrant antibacterial products in the future. The bacterial count evaluated by colony-forming units was found to be reduced with limonene-doped drug-loaded mycobacterial liposomes in comparison to those without limonene. Mechanistically, it was shown that limonene enhances membrane fluidity and influences permeability, interacting with intact bacteria and thereby improving drug delivery, which promotes greater bacterial destruction. Limonene in the antibacterial liposomal formulation was also found to enhance the release of intracellular material because of compromised membranes aiding in bacterial destruction. Finally, mycobacterial liposome formulation loaded with drugs and doped with limonene successfully eliminated Msm biofilms more effectively than either the free drug or liposomes without limonene. This clearly demonstrates the collaboration between limonene and rifampicin in combination antimycobacterial treatment.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 8","pages":"e202501110"},"PeriodicalIF":3.4,"publicationDate":"2026-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147758206","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Design and Synthesis of New Pyrazolo[1,5-c]quinazolin-5-amines as Potential TLR7/8 Modulators. 新型吡唑啉[1,5-c]喹唑啉-5胺类TLR7/8潜在调节剂的设计与合成

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-28 DOI: 10.1002/cmdc.202501053

Kushvinder Kumar, Yoshikazu Honda-Okubo, Pradeep K Das, Anshuman Dixit, Kamal Nain Singh, David A Winkler, Nikolai Petrovsky, Deepak B Salunke

{"title":"Design and Synthesis of New Pyrazolo[1,5-c]quinazolin-5-amines as Potential TLR7/8 Modulators.","authors":"Kushvinder Kumar, Yoshikazu Honda-Okubo, Pradeep K Das, Anshuman Dixit, Kamal Nain Singh, David A Winkler, Nikolai Petrovsky, Deepak B Salunke","doi":"10.1002/cmdc.202501053","DOIUrl":"https://doi.org/10.1002/cmdc.202501053","url":null,"abstract":"Multiple heterocyclic scaffolds have been found to exhibit agonist or antagonist activity at toll-like receptors (TLRs) with varying degrees of selectivity for the subtypes. TLR7 and 8 agonists are potentially valuable vaccine adjuvants while antagonists show useful activity against autoimmune diseases and cancer. A pyrazolo[1,5-c]quinazoline based compound 23, an unexplored scaffold in the domain of TLR7/8, was synthesized by analogy with lead agonists and antagonists from the literature. Compound 23 exhibited moderate agonist activity for both TLR7 and TLR8. The effect of structural modifications at the C1, C8, C9, and C10 position of the pyrazolo[1,5-c]quinazoline scaffold on hTLR7/8 activity was investigated by synthesizing a focused library of compounds. Although none of the compounds had agonist activity, three compounds were found to be dual TLR7/8 antagonists. These findings add to the existing structure-activity relationship knowledge of the tricyclic TLR7/8 modulators that will aid subsequent discovery and optimization of new drug candidates.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 8","pages":"e202501053"},"PeriodicalIF":3.4,"publicationDate":"2026-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147758249","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Mechanistic Insights Into the Photosensitizing Properties of the Topical Retinoid Tazarotene. 外用类维甲酸他沙罗汀光敏特性的机理研究。

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-28 DOI: 10.1002/cmdc.70279

Juan A Soler-Orenes, Macarena Dillon, Gemma M Rodríguez-Muñiz, Matilde Ansino-Ortiz, Inmaculada Andreu, Virginie Lhiaubet-Vallet

{"title":"Mechanistic Insights Into the Photosensitizing Properties of the Topical Retinoid Tazarotene.","authors":"Juan A Soler-Orenes, Macarena Dillon, Gemma M Rodríguez-Muñiz, Matilde Ansino-Ortiz, Inmaculada Andreu, Virginie Lhiaubet-Vallet","doi":"10.1002/cmdc.70279","DOIUrl":"https://doi.org/10.1002/cmdc.70279","url":null,"abstract":"Since the FDA approval of tretinoin in 1971, retinoids have been key in treating acne and different skin pathologies. Tazarotene (TZE), a third-generation retinoid and prodrug, is converted in the skin to its active form, tazarotenic acid (TZA). Its structure allows absorption of UVA/UVB light, prompting concerns about potential phototoxicity, but data on the excited state properties of TZE and TZA are still lacking. This work investigates these retinoids' behavior under UVA light exposure through a combined spectroscopic, analytical, and biological approximation. The results show that both compounds form long-lived triplet excited states, which interact with oxygen to produce reactive singlet oxygen. Additionally, TZA interacts with tryptophan (Trp), leading to the formation of a photoproduct with a mass corresponding to a Trp/TZA cyclobutene adduct. These results correlate with reduced cell viability in fibroblasts exposed to light after treatment with TZE or TZA, indicating potential phototoxic effects. Such light-induced reactivity may also be related to the enhanced therapeutic results observed when TZE is used alongside narrow-band UVB phototherapy.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 8","pages":"e70279"},"PeriodicalIF":3.4,"publicationDate":"2026-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13110329/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147758189","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Zwitterionic Mn(III)-Tetraphenyl Porphyrins: Water-Soluble MRI Contrast Agents with High Relaxivity 两性离子Mn(III)-四苯基卟啉：水溶性高弛豫MRI造影剂

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-16 DOI: 10.1002/cmdc.70268

Darius Ludolfs, Lennart F. V. Spickschen, Stefanie Bredehöft, Verena R. Schulze, Marie Oest, Samila Leon Chaviano, Neus Feliu, Markus Fischer, Marc-André Fortin, John V. Frangioni, Wolfgang Maison

{"title":"Zwitterionic Mn(III)-Tetraphenyl Porphyrins: Water-Soluble MRI Contrast Agents with High Relaxivity","authors":"Darius Ludolfs, Lennart F. V. Spickschen, Stefanie Bredehöft, Verena R. Schulze, Marie Oest, Samila Leon Chaviano, Neus Feliu, Markus Fischer, Marc-André Fortin, John V. Frangioni, Wolfgang Maison","doi":"10.1002/cmdc.70268","DOIUrl":"https://doi.org/10.1002/cmdc.70268","url":null,"abstract":"Manganese-based contrast agents (MBCAs) are promising alternatives to currently used gadolinium-based contrast agents (GBCAs) for magnetic resonance imaging (MRI). This study describes the synthesis and physicochemical evaluation of two new zwitterionic Mn(III) porphyrin chelates (Mn-8 and Mn-9). Both compounds were synthesized via copper-catalyzed azide–alkyne cycloaddition (CuAAC) from an azido-substituted precursor. Both zwitterionic compounds are soluble in water and are remarkably stable to acidic pH and transmetallation under challenging conditions. The complexes have a high T1-relaxivity, comparable to current clinical high-relaxivity GBCAs like gadopiclenol. In addition, zwitterionic complexes Mn-8 and Mn-9 have superior relaxivity and improved stability compared to Mn-DPDP (mangafodipir, Teslascan). The favorable properties of both compounds can be attributed to the decoration of the chelator with sulfobetaines or N-oxides. Importantly, chelation of Mn(III) by the porphyrin drastically reduces singlet oxygen generation. Mn-8 showed good contrast enhancement in vivo. These compounds are thus strong candidates for the development of next-generation gadolinium-free MRI contrast agents.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 8","pages":""},"PeriodicalIF":3.4,"publicationDate":"2026-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://chemistry-europe.onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.70268","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147686036","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Flavonoid Oxime Carbamate Derivatives: Reversal of Multidrug Resistance in Cancer Cells 类黄酮肟氨基甲酸酯衍生物：逆转癌细胞的多药耐药。

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-16 DOI: 10.1002/cmdc.202501113

Filipa Barbosa, Gabriella Spengler, Noémi Bózsity, Nikoletta Szemerédi, István Zupkó, Maria-José U. Ferreira

{"title":"Flavonoid Oxime Carbamate Derivatives: Reversal of Multidrug Resistance in Cancer Cells","authors":"Filipa Barbosa, Gabriella Spengler, Noémi Bózsity, Nikoletta Szemerédi, István Zupkó, Maria-José U. Ferreira","doi":"10.1002/cmdc.202501113","DOIUrl":"10.1002/cmdc.202501113","url":null,"abstract":"The effectiveness of cancer treatment has been seriously hindered by the development of multidrug resistance (MDR), mainly mediated by efflux transporters such as P-glycoprotein (P-gp/ABCB1). Aiming at obtaining new compounds for overcoming MDR in cancer, tangeretin (1), a natural polymethoxyflavonoid, was derivatized. After obtaining the corresponding oxime (2), a set of 23 novel oxime carbamates (3–26) was prepared via carbonyldiimidazole-mediated reaction with various amines or by reaction with isocyanates. Their structures were assigned mainly by 1D and 2D NMR experiments. The compounds (1–26) were evaluated for their MDR reversal potential, using the rhodamine-123 accumulation assay and chemosensitivity experiments, in human ABCB1-gene transfected L5178Y mouse lymphoma cells. A significant increase in P-gp inhibitory activity was observed for most of the derivatives at noncytotoxic concentrations. Notably, compounds 19, 20, and 22, bearing an aliphatic substituent, were the most active, exhibiting a strong MDR reversal effect at 2 μM. Moreover, drug combination assays revealed that most of the derivatives were able to synergize doxorubicin. Selected compounds were also tested in the ATPase assay, where most of them acted as inhibitors.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 7","pages":""},"PeriodicalIF":3.4,"publicationDate":"2026-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://chemistry-europe.onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.202501113","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147696957","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Buckybowls at the Biointerface: Sumanene and Corannulene as Emerging Platforms for Medicinal Chemistry 生物界面上的巴克碗：苏蔓烯和角环烯作为药物化学的新兴平台。

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-16 DOI: 10.1002/cmdc.202500880

Artur Kasprzak

引用次数: 0

Azo(bis)pyrazole-Ciprofloxacin Conjugates: Tuning Photopharmacological Performance Through Structural Engineering. 偶氮（双）吡唑-环丙沙星缀合物：通过结构工程调整光药理学性能。

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-14 DOI: 10.1002/cmdc.202501061

Supriya Bhunia, Santosh Kumar Jana, Debashmita Guha, Samrat Saha, Sukhendu Mandal, Subhas Samanta

{"title":"Azo(bis)pyrazole-Ciprofloxacin Conjugates: Tuning Photopharmacological Performance Through Structural Engineering.","authors":"Supriya Bhunia, Santosh Kumar Jana, Debashmita Guha, Samrat Saha, Sukhendu Mandal, Subhas Samanta","doi":"10.1002/cmdc.202501061","DOIUrl":"https://doi.org/10.1002/cmdc.202501061","url":null,"abstract":"Limiting the action of antimicrobials by employing photoswitchable antibiotics holds immense potential to combat the emergence of antimicrobial resistance. These photoswitchable antibiotics are expected to be less/nontoxic in their thermally stable states than the light-induced metastable forms, such that after treatment with the active isomer, the drug toxicity will be automatically reduced or drastically lost after excretion from human and animal bodies into the environment. However, the design of such light-sensitive antibiotics has proven to be very challenging. Most of the previously reported azo-based ciprofloxacin derivatives exhibited diminished potency with the light-induced cis state. Herein, we present the design and synthesis of azoheteroarene-ciprofloxacin conjugates, which exhibited higher antimicrobial potency by the cis-isomer than the trans-isomer against Gram-positive and Gram-negative pathogens. The potency was tuned by varying molecular design. All conjugates displayed a high degree of bidirectional photoisomerization, long cis half-lives, and impressive photofatigue resistance. Notably, the conjugate AAP-2-Cip carrying a flexible linker and pyrazole at the exterior of arylazopyrazole furnished the highest activity difference of 2.5-fold between two isomers, and the cis isomer of ABP-Cip showed 1.7-fold increased potency than ciprofloxacin. Docking studies revealed different binding affinities for two isomers with the DNA gyrase. The molecular design concept unfolded herein may be applied to other antibiotics to transform them into potent photoswitchable antibiotics for suppressing the growth of antibiotic-resistant pathogens.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 7","pages":"e202501061"},"PeriodicalIF":3.4,"publicationDate":"2026-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147715376","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Metalloids: Semi as Metals yet Full of Antimicrobial Potential. 类金属：半金属但充满抗菌潜力。

IF 3.4 4区医学

ChemMedChem Pub Date : 2026-04-14 DOI: 10.1002/cmdc.202500979

Kevin Böhm, Muhammad Jawad Nasim, Claus Jacob

{"title":"Metalloids: Semi as Metals yet Full of Antimicrobial Potential.","authors":"Kevin Böhm, Muhammad Jawad Nasim, Claus Jacob","doi":"10.1002/cmdc.202500979","DOIUrl":"10.1002/cmdc.202500979","url":null,"abstract":"In the periodic table, the metalloids boron (B), silicon (Si), germanium (Ge), arsenic (As), antimony (Sb), and tellurium (Te) demarcate a borderline between the metals and non-metals. Also referred to as semi-metals, their behaviour is indeed characterized by inorganic ions, organometallic complexes, and covalent compounds. Yet despite this unique medley of inorganic and organic molecules, reactivities and activities, and century-old traditional uses, their pharmaceutical applications today are often underestimated or associated with outright toxicity. Still, recent research has taken a closer look at (some of) these elements and has encountered an amazing assortment of natural metalloid-containing products, many with distinct antimicrobial activities. At the same time, metalloid-containing complexes have been synthesized and tested successfully as ionophores, in ligand-exchange reactions with amino acids, such as cysteine, or as redox modulators triggering oxidative stress. This has been complemented by an extensive synthesis of organic metalloid-based compounds, even including bioisosteric replacements for carbon. Today, a few metalloid compounds are still or already used in therapy; others are in clinical trials, and many more are in the pipeline, clearly demanding full attention for the semi-metals and their many colourful compounds.","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"21 7","pages":"e202500979"},"PeriodicalIF":3.4,"publicationDate":"2026-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13091928/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147715413","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0