Bioorganic & Medicinal Chemistry Letters最新文献

{"title":"Synthesis and anti-breast cancer evaluation of new bakuchiol derivatives.","authors":"Hong-Mei Li, Jing Zhu, Ke Zhong, Jie Chen, Long Zhao, Zhen-Hai Zhang, Cheng-Zhu Wu","doi":"10.1016/j.bmcl.2025.130361","DOIUrl":"10.1016/j.bmcl.2025.130361","url":null,"abstract":"<p><p>In this study, we semi-synthesized nineteen new derivatives of bakuchiol and evaluated their anti-breast cancer properties. Among them, compound 19 stood out as the most effective demonstrating significant cytotoxic activity against MDA-MB-231 cells, with IC₅₀ values of 4.13 μM. Notably, the cytotoxicity of compound 19 towards normal mouse hepatocytes (Aml-12) cells was considerably lower, with IC₅₀ values of 31.60 μM. Our findings indicated that compound 19 triggered apoptosis in MDA-MB-231 cells by increasing the levels of Bax and Cyt C, reducing Bcl-2, and initiating caspase-3 cleavage. It also suppressed the invasion and migration of MDA-MB-231 cells by down-regulating MMP-2 and MMP-9 expression and up-regulating E-cadherin protein levels. We further demonstrated that compound 19 significantly suppressed tumor growth in nude mice xenografted with MDA-MB-231 cells.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130361"},"PeriodicalIF":2.2,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144797759","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}

{"title":"Discovery and structural-activity relationship of N-benzyl-2-fluorobenzamides as EGFR/HDAC3 dual-target inhibitors for the treatment of triple-negative breast cancer.","authors":"Gong-Hui Ge, Shuai Guo, Ting-Ting Li, Yan-Ping Wang, Li-Rong Liu, Wen-Hui Yu, Hao Hu, Yi-Meng Zheng, Jing-Han Yan, Ying-Hao Sun, Jing-Wei Liang, Fan-Hao Meng, Ting-Jian Zhang","doi":"10.1016/j.bmcl.2025.130362","DOIUrl":"10.1016/j.bmcl.2025.130362","url":null,"abstract":"<p><p>Epidermal growth factor receptor (EGFR) and histone deacetylase 3 (HDAC3) synergistically drive malignant progression in triple-negative breast cancer (TNBC). In this study, a series of N-benzyl-2-fluorobenzamide derivatives (11-43) were identified as EGFR/HDAC3 dual-target inhibitors. Among them, compound 38 exhibited the most promising activity, with IC₅₀ values of 20.34 nM and 1.09 μM against EGFR and HDAC3, respectively. Molecular modeling revealed that the 2-fluorobenzamide moiety of 38 chelates with Zn²⁺ in the active channel of HDAC3, while the 4-fluorobenzyl group occupies the ATP-binding pocket of EGFR, exercising a dual-target binding function. In vitro experiments demonstrated that 38 exhibited superior anti-proliferative activity (IC₅₀ = 1.98 μM) against MDA-MB-231 cells compared to chidamide (IC₅₀ = 24.37 μM), inducing 74.15 % inhibition of cell migration and 57.4 % late-stage apoptosis. In vivo studies revealed that 38 (30 mg/kg/day) suppressed tumor growth by 34.78 % without significant toxicity. Collectively, 38 represents a novel dual EGFR/HDAC3 inhibitor that shows promising potential for providing new therapeutic insights into TNBC treatment.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130362"},"PeriodicalIF":2.2,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144787866","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}

{"title":"Synthesis of pisiferic acid analogues and their anti-adipogenic effect in 3T3-L1 adipocytes.","authors":"Ayako Oshika, Sayumi Ono, Haruka Iwano, Manami Toda, Risa Obayashi, Yuna Takagi, Mako Higashitani, Satomi Fukuoka, Miduki Furukawa, Karen Yagami, Rena Okamura, Natsumi Futoi, Hiroki Yoshioka, Reiko Yano, Koji Yoshida, Hyun-Sun Park, Tomoyo Hasuda, Yukio Hitotsuyanagi, Koichi Takeya, Tomohiro Yamaguchi, Yutaka Aoyagi","doi":"10.1016/j.bmcl.2025.130354","DOIUrl":"10.1016/j.bmcl.2025.130354","url":null,"abstract":"<p><p>12-O-alkyl, acyl, and phenylcarbamoyl, and 11-bromo-7-oxo analogues were prepared from pisiferic acid from Chamaecyparis pisifera, and evaluated anti-adipogenic activity. Among them, pisiferic acid and methyl 12-O-phenylcarbamoylpisiferic acid methyl ester showed relatively high anti-adipogenic effect in 3T3-L1 adipocytes and should be thought to be potential candidates for anti-obesity drug.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130354"},"PeriodicalIF":2.2,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144793047","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}

{"title":"Efficient synthesis, stability-guided optimization and anti-ulcerative colitis evaluation of bee venom peptide melittin.","authors":"Cheng-Jian Pang, Jing-Fang Yao, Qiu-Lan Lv, Li-Ze Zhang, Qian-Yao Yu, Li Zeng, Yun-Kun Qi","doi":"10.1016/j.bmcl.2025.130357","DOIUrl":"10.1016/j.bmcl.2025.130357","url":null,"abstract":"<p><p>Ulcerative colitis (UC) is considered as one of the most prevalent inflammatory bowel diseases (IBDs), which increases risks for colectomy and colorectal cancer. However, due to moderate efficiency and potential side effects of first-line drugs, it is desirable to develop more efficient anti-UC agents. The natural peptide Melittin, which is the main active ingredient of bee venom, is considered as a potential scaffold for the development of anti-UC drugs. Nevertheless, as a linear amphipathic peptide, Melittin could be degraded by various proteases, suffering from poor stability and short half-lives. Previous studies on structural optimization or the potential of Melittin-derived peptides for anti-UC applications still remain limited. In this study, the stability-guided optimization and anti-UC evaluation were conducted on Melittin. The robust synthetic strategy, in vivo anti-UC activity, and anti-inflammatory mechanism were investigated. Compared with Melittin, the derived peptides represented by PCJ-675 were found to exhibit improved proteolytic stability. In the dextran sulfate sodium (DSS)-induced UC mice model, PCJ-675 could significantly alleviate both colon shortening and suppress inflammation symptoms in colon tissue. The western blotting and biochemical indicators suggested that the oral administration of PCJ-675 could protect the colon in colitis mice by inhibiting both the excessive activation of the inflammation-related TLR4/NF-κB pathway and the overexpression of pro-inflammatory cytokines (eg, IL-1β, IL-6, and TNF-α). Collectively, this study not only stablished robust strategies to improve the stability and anti-UC potential of Melittin, but also provided valuable references for the future development of natural cytotoxic peptides based anti-UC agents.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130357"},"PeriodicalIF":2.2,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144783122","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}

{"title":"¹¹C-labeling of 20(S)-protopanaxadiol, an aglycon of ginsenoside, based on the use of Pd(0)-mediated rapid C-[¹¹C]methylation of boronic precursors.","authors":"Yoshiki Ooshima, Hiroko Koyama, Aya Ogata, Hiroshi Ikenuma, Takashi Yamada, Hiroyuki Kojima, Takashi Kato, Yasuyuki Kimura, Masaaki Suzuki","doi":"10.1016/j.bmcl.2025.130356","DOIUrl":"10.1016/j.bmcl.2025.130356","url":null,"abstract":"<p><p>Ginsenosides, the pharmacologically active components of Panax ginseng, are widely used in herbal medicine and reportedly exert diverse biological effects, including anticancer, anti-inflammatory, and neuroprotective activities. However, their pharmacological mechanisms remain poorly understood, owing to the lack of chemical probes suitable for in vivo analyses. Herein, we report the development of a ¹¹C radiolabeling of 20(S)-protopanaxadiol (PPD), a major aglycone-type active ginsenoside metabolite, for positron emission tomography (PET) imaging. For the ¹¹C labeling of PPD, we focused on the terminal vinyl methyl group of the dammarane-type triterpene backbone, a common structural element found in ginsenosides. A boronic precursor applicable for rapid ¹¹C-methylation was efficiently synthesized via steps focusing on the controlled cross-metathesis of an internal olefin. The subsequent Pd(0)-mediated rapid ¹¹C-methylation was conducted in N,N-dimethylformamide (DMF)/H₂O using [Pd₂(dba)₃], P(o-tolyl)₃, and sodium ascorbate, which functioned as a base and a radical scavenger. After formulation, the resulting [¹¹C]PPD was obtained in a decay-corrected radiochemical yield of 15 ± 2 % (n = 3), with a total radioactivity of 1.0 ± 0.3 GBq (n = 3) and molar activity of 124 ± 7 GBq/μmol (n = 3). Radiochemical purity was ≥99 %, and the total synthesis time was 29 min. Using [¹¹C]PPD, PET imaging of the brains of healthy rats and abdomens of healthy mice demonstrated low brain uptake and pronouncedly clear hepatobiliary excretion of radiolabeled species. These findings may provide a foundation for the general labeling of ginsenoside structures with ¹¹C radioisotopes, thereby enabling systematic in vivo pharmacokinetic analyses of PPD derivatives to advance ginsenoside-based drug development.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130356"},"PeriodicalIF":2.2,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144774419","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}

{"title":"Synthesis and antitumor activities of quaternary carbon-containing selenolactones.","authors":"Danqing Li, Yumiao Zhen, Ran Tang, Boying Wang, Haijing Zhong, Xiaojian Jiang, Ying-Yeung Yeung","doi":"10.1016/j.bmcl.2025.130439","DOIUrl":"https://doi.org/10.1016/j.bmcl.2025.130439","url":null,"abstract":"<p><p>The cytotoxicity of α-exo-methylene-lactones has been extensively studied. However, further study of the α-exo-methylene-lactones for anticancer application was hampered primarily by its poor selectivity and solubility. In the present work, a series of α-exo-methylene-selenolactone derivatives bearing amine substituent, selenium functionality and quaternary carbon center were synthesized and evaluated for their anticancer activities. The most potent compound, 2d, was about 9-fold more selective for cancer cells than normal cells. Moreover, 2d significantly inhibited tumor growth in mouse xenograft model and had no observable toxic effect.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130439"},"PeriodicalIF":2.2,"publicationDate":"2025-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145342480","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}

{"title":"Discovery of a novel pharmacokinetic booster: A small intestine-selective CYP3A4 inhibitor with dibenzyl ether structure.","authors":"Shoki Hoshikawa, Koki Kimura, Chisaki Hanada, Yukiko Karuo, Atsushi Tarui, Kazuyuki Sato, Masaaki Omote, Makoto Kataoka, Kentaro Kawai","doi":"10.1016/j.bmcl.2025.130445","DOIUrl":"https://doi.org/10.1016/j.bmcl.2025.130445","url":null,"abstract":"<p><p>This study describes the development of novel dibenzyl ether derivatives that selectively inhibit intestinal CYP3A4 and are expected to function as pharmacokinetic boosters. Based on previously reported phenylazole derivatives, new compounds were synthesized by systematically modifying the azole moiety, linker structure, and ester functionality to explore structure-activity relationships. The selected dibenzyl ether derivatives exhibited potent CYP3A4 inhibitory activity and remained stable in the presence of intestinal S9 fractions, whereas they were rapidly metabolized in liver S9 fractions to form less active metabolites. The ability to undergo rapid hepatic metabolism is considered advantageous for reducing the risk of drug-drug interactions. These findings suggest that the dibenzyl ether derivatives represent a promising lead for the development of intestine-selective pharmacokinetic booster candidates.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130445"},"PeriodicalIF":2.2,"publicationDate":"2025-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145342479","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}

{"title":"Coumarin-benzimidazole hybrids: Design, synthesis and identification of potential anticancer agents.","authors":"C G Arya, Neethu Mariam Thomas, Munugala Chandrakanth, Anoop Kallingal, P G Amrutha, M S Sivapriya, Ramesh Gondru, Janardhan Banothu","doi":"10.1016/j.bmcl.2025.130444","DOIUrl":"10.1016/j.bmcl.2025.130444","url":null,"abstract":"<p><p>A series of coumarin-benzimidazole conjugates (6a-p) was designed and synthesized via a polyphosphoric acid (PPA)-mediated condensation of o-phenylenediamine derivatives with coumarin-3-carboxylic acids. The in vitro anticancer activity of all conjugates was evaluated against lung (A549) and breast (MCF7) cancer cell lines. Except for hybrids 6l (A549) and 6c (MCF7), all compounds exhibited notable cytotoxicity toward both cell lines, with IC₅₀ values ranging from 0.85 ± 0.07 to 48.01 ± 0.45 μM. Among them, the unsubstituted derivative 6b emerged as the most potent compound, showing IC₅₀ values of 0.85 ± 0.07 μM (A549) and 1.90 ± 0.08 μM (MCF7). Compounds 6a, 6c, and 6g also demonstrated strong activity against A549 cells, with IC₅₀ values of 1.86 ± 0.19 μM, 1.05 ± 0.09 μM, and 2.23 ± 0.13 μM, respectively. Furthermore, the potent conjugates 6b and 6g were found to be non-toxic toward Vero cells (LD₅₀ > 100 μM), indicating selective cytotoxicity toward cancer cells. In silico molecular docking studies suggested that the activity of compound 6b against both cell lines may result from inhibition of sphingosine kinase 1 (SK1), whereas the potency of 6g against A549 cells could be attributed to cyclin-dependent kinase 2 (CDK2) inhibition. These computational predictions warrant further validation through target-specific biological assays. ADMET analysis further revealed that conjugate 6b possesses favorable pharmacokinetic properties, supporting its potential as a promising lead for future anticancer drug development.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130444"},"PeriodicalIF":2.2,"publicationDate":"2025-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145336141","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}

{"title":"Inflammation and diabetic inhibitors from Amanita abrupta and Amanita pantherina: experimental and computational results","authors":"Dao C. To ,&nbsp;Minh Q. Pham ,&nbsp;Phuong D.N. Nguyen ,&nbsp;Phi H. Nguyen ,&nbsp;Huu T. Nguyen ,&nbsp;Viet T. Trinh ,&nbsp;Le M. Hoang ,&nbsp;Hoa T. Nguyen ,&nbsp;Thi V.H. Truong","doi":"10.1016/j.bmcl.2025.130438","DOIUrl":"10.1016/j.bmcl.2025.130438","url":null,"abstract":"<div><div>This study investigates potential inhibitors of nitric oxide (NO) production, <em>α</em>-glucosidase, and protein tyrosine phosphatase 1B (PTP1B) from <em>Amanita abrupta</em> and <em>Amanita pantherina</em>. Sixteen compounds (<strong>1</strong>–<strong>16</strong>) were isolated by chromatographic techniques and high-performance liquid chromatography (HPLC), and their structures were elucidated by nuclear magnetic resonance (NMR) and literature comparison. Biological activities were evaluated <em>via in vitro</em> assays: the Griess assay for NO inhibition, the <em>p</em>-nitrophenol assay for <em>α</em>-glucosidase, and enzymatic assays for PTP1B. Molecular docking was employed to investigate protein–ligand interactions. The isolates included alanine (<strong>1</strong>), threonine (<strong>2</strong>), 2-amino-4-pentynoic acid (<strong>3</strong>), 4-hydroxy-2-pyrrolidinone (<strong>4</strong>), ibotenic acid (<strong>5</strong>), serotonin (<strong>6</strong>), uracil (<strong>7</strong>), hypoxanthine (<strong>8</strong>), bufotenine (<strong>9</strong>), <em>β</em>-sitosterol (<strong>10</strong>), stigmasterol (<strong>11</strong>), cycloeucalenol (<strong>12</strong>), spinasterol (<strong>13</strong>), daucosterol (<strong>14</strong>), stigmasterol-3-O-<em>β</em>-D-glucoside (<strong>15</strong>), and betulin (<strong>16</strong>). Compounds <strong>1</strong> and <strong>2</strong> exhibited weak NO inhibition (IC₅₀ = 68.76 and 52.47 μM). Compound <strong>14</strong> displayed the strongest <em>α</em>-glucosidase inhibition (IC₅₀ = 10.56 μM), while compounds <strong>10</strong>–<strong>13</strong> and <strong>16</strong> showed moderate effects (IC₅₀ = 19.52–32.14 μM). Serotonin (<strong>6</strong>) also had moderate activity (IC₅₀ = 78.23 μM). For PTP1B inhibition, betulin (<strong>16</strong>) was most potent (IC₅₀ = 16.80 μM), followed by compounds <strong>10</strong>, <strong>11</strong>, and <strong>13</strong> with weaker activities (IC₅₀ = 36.28–48.17 μM). Overall, selected compounds (<strong>1</strong>, <strong>2</strong>, <strong>10</strong>–<strong>14</strong>, and <strong>16</strong>) exhibited promising bioactivities, warranting further docking studies against inducible nitric oxide synthase (iNOS), PTP1B, and 3AJ7. ADMET (absorption, distribution, metabolism, excretion, and toxicity) predictions supported favorable pharmacokinetic properties and potential drug-likeness, highlighting these molecules as leads for anti-inflammatory and anti-diabetic drug discovery.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"131 ","pages":"Article 130438"},"PeriodicalIF":2.2,"publicationDate":"2025-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145306457","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}

{"title":"Improved synthesis and anti-inflammatory activity of new fluorinated dihydropyranonaphthoquinone compounds","authors":"Quynh Giang Nguyen Thi ,&nbsp;Ha Thanh Nguyen ,&nbsp;Tuyet Anh Dang Thi ,&nbsp;Kieu Trinh Nguyen Thi ,&nbsp;Giang Le-Nhat-Thuy ,&nbsp;Phuong Hoang Thi ,&nbsp;Tuan Anh Nguyen ,&nbsp;Mai Dang Thi ,&nbsp;Ha Nguyen Thi Thu ,&nbsp;Hoang Sa Nguyen ,&nbsp;Tuyen Van Nguyen","doi":"10.1016/j.bmcl.2025.130434","DOIUrl":"10.1016/j.bmcl.2025.130434","url":null,"abstract":"<div><div>This study presents the synthesis of new fluorinated dihydropyranonapthoquinone compounds by means of microwave-prompted four-component reactions using lawson, fluorinated aromatic aldehydes, ethyl 4,4,4-trifluoroacetoacetate and ammonium acetate. The products were thoroughly characterized by spectroscopic methods and assessed for their anti-inflammatory activity in lipopolysaccharide-stimulated RAW264.7 macrophage cells. All synthesized compounds demonstrated notable inhibitory effects on NO production with IC₅₀ ranging from 1.67 ± 0.02 to 28.81 ± 2.44 μM without causing significant toxicity. Interestingly, compound <strong>8n</strong> showed the most potent NO inhibitory activity in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells with IC₅₀ value of 1.67 ± 0.02 μM. Moreover, compounds <strong>8c,</strong><strong>h,i,l</strong> significantly decreased the levels of pro-inflammatory cytokines IL-1β and IL-6 in LPS-stimulated RAW264.7 macrophages. These results indicate the potential of these compounds as promising candidates for the development of new anti-inflammatory agents.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"130 ","pages":"Article 130434"},"PeriodicalIF":2.2,"publicationDate":"2025-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145285395","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}