RSC medicinal chemistry最新文献

{"title":"Metal-free synthesis of N-fused quinazolino-quinazoline-diones as a <i>MALAT1</i> RNA triple helix intercalator.","authors":"Vijay Babu Pathi, Pranotosh Das, Abhyuday Guin, Manish Debnath, Biswadip Banerji","doi":"10.1039/d4md00614c","DOIUrl":"10.1039/d4md00614c","url":null,"abstract":"<p><p>The development of chemical scaffolds that target highly conserved <i>MALAT1</i> RNA received attention due to its significance in splicing, nuclear organization, and gene expression in disease progression pathways. Here, we synthesized a series of N-fused quinazolino-quinazoline-diones <i>via</i> a PIDA-induced C-N coupling methodology to target <i>MALAT1</i>. Interestingly, compound 2z binds to the UUG pocket of a <i>MALAT1</i> RNA triple-helix through intercalation, evidenced from molecular docking studies, fluorescence-based assay and CD experiments. 2z exhibited cytotoxicity towards <i>MALAT1</i> overexpressing cancer cells (SKOV-3, IC₅₀ of 8.0 ± 0.4 μM). These findings demonstrated 2z as a <i>MALAT1</i> RNA triple-helix intercalator with therapeutic potential, offering an important chemical scaffold to understand <i>MALAT1</i> activity in disease development pathways.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11537285/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142590945","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}

{"title":"Synthesis of cationic <i>N</i>-acylated thiazolidine for selective activity against Gram-positive bacteria and evaluation of <i>N</i>-acylation's role in membrane-disrupting activity.","authors":"Aleena Pious, Vignesh Venkatasubramanian, Dharshini Karnan Singaravelu, Subburethinam Ramesh, Fuad Ameen, Anbazhagan Veerappan","doi":"10.1039/d4md00626g","DOIUrl":"10.1039/d4md00626g","url":null,"abstract":"<p><p>The evolution of antimicrobial-resistant strains jeopardizes the existing clinical drugs and demands new therapeutic interventions. Herein, we report the synthesis of cationic thiazolidine bearing a quaternary pyridinium group, in which thiazolidine was <i>N</i>-acylated with fatty acid to establish a hydrophilic-lipophilic balance that disrupts bacterial membranes. The bacterial growth inhibition assays and hemolytic activity against human red blood cells indicate that the <i>N</i>-acylated cationic thiazolidine (QPyNATh) inhibits Gram-positive bacteria at lower minimum inhibitory concentrations (MIC) and is selective for bacteria over mammalian cells. <i>N</i>-Acylation modulates MIC, and it is found that the <i>N</i>-palmitoylated compound, QPyN16Th, had the lowest MIC (1.95 μM) against Gram-positive, <i>Enterococcus faecalis</i>, <i>Staphylococcus aureus</i> and methicillin-resistant <i>Staphylococcus aureus</i> (MRSA). In contrast, the <i>N</i>-myristoylated compound, QPyN14Th, showed the lowest MIC (31.25 μM) against Gram-negative, <i>Escherichia coli</i>, uropathogenic <i>Escherichia coli</i>, and <i>Pseudomonas aeruginosa</i>. At 1× MIC, QPyNATh permeabilizes the bacterial membrane, depolarizes the cytoplasmic membranes, and produces excess reactive oxygen species to kill the bacteria, as evidenced by live and dead staining. Interestingly, only QPyNATh containing a palmitoyl acyl chain demonstrated membrane-damaging activity at 2 μM concentrations, suggesting that the optimal hydrophilic-lipophilic balance enables QPyN16Th to selectively kill Gram-positive bacteria at lower doses. <i>S. aureus</i> develops resistance to ciprofloxacin quickly; however, no resistance to QPyN16Th is observed after several passages. As a proof of concept, the animal study revealed that QPyN16Th treatment reduced the bacterial burden in MRSA-infected zebrafish, allowing them to recover from infection and resume normal life. The results imply that lipidation and derivatizing thiazolidine with cationic charge offer an antimicrobial that is selective to treat Gram-positive bacterial infections, biocompatible, and less prone to develop resistance.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11537284/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142590949","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}

{"title":"A novel approach for the synthesis of the cyclic lipopeptide globomycin.","authors":"Samantha J Bann, Stephen A Cochrane","doi":"10.1039/d4md00685b","DOIUrl":"10.1039/d4md00685b","url":null,"abstract":"<p><p>Cyclic lipopeptides (CLiPs) are a highly diverse class of secondary metabolites produced by bacteria and fungi. Examples of CLiPs have been found that possess potent antimicrobial activity against multidrug-resistant Gram-negative bacteria. Globomycin is a 19-membered CLiP that kills both Gram-positive and Gram-negative bacteria through inhibition of lipoprotein signal peptidase II (Lsp). It can only be obtained in small quantities from its <i>Streptomyces</i> producer strain, so there has been much interest in development of synthetic methods to access globomycin and analogues. Globomycin contains an N-terminal anti-α-methyl-β-hydroxy nonanoyl lipid tail, whose hydroxyl group forms an ester with the C-terminal carboxylate. Constructing the anti-arrangement between the α-methyl and β-hydroxy is synthetically challenging and previous globomycin syntheses are not compatible with diversification of the lipid tail after the stereocenters have been installed. Herein, we describe a new approach for the synthesis of globomycin that allows for facile lipid diversification. Using an anti-Evans Aldol condensation, a common intermediate is obtained that allows different \"lipid swapping\" through Grubbs-catalyzed cross-metathesis. Upon auxiliary cleavage, the resulting lipid can then be utilized in solid-phase peptide synthesis. Given the plethora of lipopeptides that contain β-hydroxy lipids, this method offers a convenient approach for convergent generation of lipopeptide analogues.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11528322/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142568166","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}

{"title":"Miniaturized click chemistry and direct screening facilitate the discovery of triazole piperazine SARS-CoV-2 M^pro inhibitors with improved metabolic stability.","authors":"Shenghua Gao, Letian Song, Bing Ye, Mianling Yang, Junyi Li, Manyu Gu, Ann E Tollefson, Karoly Toth, Peng Zhan, Xinyong Liu","doi":"10.1039/d4md00555d","DOIUrl":"10.1039/d4md00555d","url":null,"abstract":"<p><p>The continuous mutational nature of SARS-CoV-2 and its inter-species' similarities emphasize the urgent need to design and develop more direct-acting antiviral agents against highly infectious variants. Herein, we report on the efficient discovery of potent non-covalent non-peptide-derived M^pro inhibitors using miniaturized click chemistry and direct screening. Based on the privileged piperazine scaffold, 68 triazole-containing derivatives were assembled and screened. Notably, representative compound C1N46 (IC₅₀ = 1.87 μM, EC₅₀ = 6.99 μM, CC₅₀ > 100 μM) displayed potent inhibition activity against M^pro and showed promising anti-SARS-CoV-2 properties <i>in vitro</i>. Additionally, C1N46 exhibited improved liver microsome stability compared to lead compound GC-14. Docking studies predicted a multi-site binding mode of the triazole-based compounds. In conclusion, our studies validate the efficacy and feasibility of click chemistry in rapidly discovering antiviral agents.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11528906/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142568512","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}

{"title":"Synthesis and biological evaluation of novel D-ring fused steroidal <i>N</i>(2)-substituted-1,2,3-triazoles.","authors":"Branislava Tenjović, Sofija Bekić, Andjelka Ćelić, Edward Petri, Julia Scholda, Florian Kopp, Marija Sakač, Andrea Nikolić","doi":"10.1039/d4md00297k","DOIUrl":"10.1039/d4md00297k","url":null,"abstract":"<p><p>In this study, a series of 13 new D-ring fused steroidal <i>N</i>(2)-substituted-1,2,3-triazoles were synthesized, characterized and evaluated for their biological activities. The relative binding affinities of the synthesized compounds for the ligand-binding domains of estrogen receptors α and β, androgen receptor and glucocorticoid receptor demonstrated that androstane derivatives 3a and 3h and estratriene derivative 4e showed highly specific and strong binding affinity for estrogen receptor β, while 3b, 3e, 4a and 4b displayed high binding affinity for the glucocorticoid receptor. The synthesized compounds were tested for their ability to inhibit aldo-keto reductases 1C3 and 1C4 <i>in vitro</i> by monitoring NADPH consumption using fluorescence spectroscopy. The most potent aldo-keto reductase 1C3 inhibitors were compounds 3h (71.17%) and 3f (69.9%). Moreover, a molecular docking study was carried out for compounds 3f and 3h against aldo-keto reductase 1C3 and results showed that compounds 3h and 3f could bind in the same site and orientation as EM1404. However, polar atoms in the triazole group enable additional hydrogen bonding deeper in SP1 with Tyr319, Tyr216 and the NADP⁺ cofactor, which are not visible in the AKR1C3-EM1404 crystal structure. The synthesized compounds were screened for their anticancer activity against four cancer cell lines. Compound 3f demonstrated moderate toxic effects across various cancer types, while displaying lower toxicity towards the healthy cell line. In summary, our findings indicate that <i>N</i>(2)-substituted-1,2,3-triazoles are high-affinity ligands for estrogen receptor β and glucocorticoid receptor, inhibitors of aldo-keto reductase 1C3 enzyme, and exhibit antiproliferative effects against cancer cells, suggesting that they could serve as scaffolds for anticancer drug development.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11488686/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142473778","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}

{"title":"Advances in antibacterial agents for <i>Mycobacterium fortuitum</i>.","authors":"Carlos Roberto Tavolari Jortieke, Angélica Rocha Joaquim, Fernando Fumagalli","doi":"10.1039/d4md00508b","DOIUrl":"10.1039/d4md00508b","url":null,"abstract":"<p><p><i>Mycobacterium fortuitum</i> is an emerging human pathogen, characterized by an increase in prevalence and antibacterial resistance over the years, highlighting the need for the development of new drugs against this rapidly growing nontuberculous mycobacterium (NTM). To support this crusade, this review summarizes findings from the past two decades concerning compounds with antimycobacterial activity against <i>M. fortuitum</i>. It identifies the most promising and effective chemical frameworks to inspire the development of new therapeutic alternatives for infections caused by this microorganism. Most compounds effective against <i>M. fortuitum</i> are synthetic, with macozinone, featuring a 2-piperazine-benzothiazinone framework, standing out as a notable drug candidate. Among natural products, the polyphenolic polyketide clostrubin and the sansanmycin peptide analogs have shown efficacy against this NTM. Some compounds' mechanisms of action on <i>M. fortuitum</i> have been studied, including NITD-916, which acts as an enoyl-acyl carrier protein reductase inhibitor, and TBAJ-5307, which inhibits F-ATP synthase. Moreover, this review discusses the pathogenic molecular mechanisms and potential therapeutic targets within this mycobacterium.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11528911/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142568297","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}

{"title":"Design, synthesis, and structure-activity relationship studies of 6<i>H</i>-benzo[<i>b</i>]indeno[1,2-<i>d</i>]thiophen-6-one derivatives as DYRK1A/CLK1/CLK4/haspin inhibitors.","authors":"Abdelfattah Faouzi, Alexandre Arnaud, François Hallé, Jean Roussel, Mandy Aymard, Vincent Denavit, Cong Viet Do, Angélique Mularoni, Mohamed Salah, Ahmed ElHady, Thanh-Nhat Pham, Alexandre Bancet, Marc Le Borgne, Raphaël Terreux, Roland Barret, Matthias Engel, Thierry Lomberget","doi":"10.1039/d4md00537f","DOIUrl":"10.1039/d4md00537f","url":null,"abstract":"<p><p>A series of sulfur-containing tetracycles was designed and evaluated for their ability to inhibit protein kinase DYRK1A, a target known to have several potential therapeutic applications including cancers, Down syndrome or Alzheimer's disease. Our medicinal chemistry strategy relied on the design of new compounds using ring contraction/isosteric replacement and constrained analogy of known DYRK1A inhibitors, thus resulting in their DYRK1A inhibitory activity enhancement. Whereas a good inhibitory effect of targeted DYRK1A protein was observed for 5-hydroxy compounds 4i-k (IC₅₀ = 35-116 nM) and the 5-methoxy derivative 4e (IC₅₀ = 52 nM), a fairly good selectivity towards its known DYRK1B off-target was observed for 4k. In addition, the most active compound 4k, having an ATP-competitive mechanism of action, proved to be also a potent inhibitor of CLK1/CLK4 (IC₅₀ = 20 and 26 nM) and, to a lesser extent, of haspin (IC₅₀ = 76 nM) kinases. <i>In silico</i> docking studies within the DYRK1A, CLK1/CLK4 and haspin ATP binding sites were carried out to understand the interactions of our tetracyclic derivatives 4 with these targets. Antiproliferative activities on U87/U373 glioblastoma cell lines of the most potent compound 4k showed a moderate effect (IC₅₀ values between 33 and 46 μM). Microsomal stabilities of the designed compounds 4a-m were also investigated, showing great disparities, depending on benzo[<i>b</i>]thiophene ring 5-substitution.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11487425/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142473768","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}

{"title":"Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity.","authors":"Poorvi Saraf, Bhagwati Bhardwaj, Akash Verma, Mohammad Aquib Siddiqui, Himanshu Verma, Pradeep Kumar, Samridhi Srivastava, Sairam Krishnamurthy, Saripella Srikrishna, Sushant Kumar Shrivastava","doi":"10.1039/d4md00471j","DOIUrl":"10.1039/d4md00471j","url":null,"abstract":"<p><p>Piperazine derivatives were screened using the ChEMBL database, paving the way for the design, synthesis, and evaluation of a novel series of dual COX-2/5-LOX inhibitors and identifying their role in mitigating cancer cell proliferation. Compound 9d with 4-Cl substitution at the terminal phenyl ring showed promising inhibition of COX-2 (IC₅₀ = 0.25 ± 0.03 μM) and 5-LOX (IC₅₀ = 7.87 ± 0.33 μM), outperforming the standards celecoxib (IC₅₀ = 0.36 ± 0.023 μM) and zileuton (IC₅₀ = 14.29 ± 0.173 μM), respectively. The two most active derivatives 9d and 9g indicated a significant anti-inflammatory response in a paw edema model by inhibiting PGE2, IL-6, and TNF-α and an increase in IL-10 concentrations. Interestingly, 9d effectively reduced pain by 55.78%, closely comparable to the 59.09% exhibited by the standard indomethacin, and was also devoid of GI, liver, kidney, and cardiac toxicity. Furthermore, 9d demonstrated anti-cancer potential against <i>in vitro</i> A549, COLO-205, and MIA-PA-CA-2 human cancer cell lines and an <i>in vivo Drosophila</i> cancer model. The pharmacokinetic investigations revealed that 9d has good oral absorption characteristics.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11487423/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142473753","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}

{"title":"Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors.","authors":"Chunfei Zhang, Yixin Liu, Xiao Zhang, Chunping Wan, Zewei Mao","doi":"10.1039/d4md00621f","DOIUrl":"10.1039/d4md00621f","url":null,"abstract":"<p><p>Cancer is one of the most significant public health problems worldwide, and the discovery and development of efficient VEGFR-2 inhibitors has been a research hotspot in cancer treatment. In the present work, a series of novel benzofuran-based chalcone derivatives have been prepared, and <i>in vitro</i> anti-tumor activities of them have been evaluated. The results indicated that the compounds displayed potent anticancer activity against HCC1806, HeLa and A549 cell lines. The preliminary mechanism study showed that 4g could effectively induce the apoptosis of HCC1806 cells, and showed inhibitory effect on VEFGR-2. The molecular docking study indicated that 4g had an obvious binding site with the target VEGFR-2 (PDB ID: 4BSK). Therefore, the benzofuran-based chalcone derivatives could be considered as potent VEGFR-2 inhibitors.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11528908/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142568707","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}

{"title":"S-MGBs bearing amidine tail groups are potent, selective antiplasmodial agents.","authors":"Marina Perieteanu, Tayner Rodriguez Garzon, Leah M C McGee, Abedawn I Khalaf, Colin J Suckling, Rebecca Beveridge, Vicky M Avery, Fraser J Scott","doi":"10.1039/d4md00619d","DOIUrl":"10.1039/d4md00619d","url":null,"abstract":"<p><p>There were an estimated 249 million cases of malaria globally in 2022, causing approximately 608 000 deaths. Most of these are attributed to infection by <i>P. falciparum</i>. Strathclyde minor groove binders (S-MGBs) are a promising new class of anti-infective agent that have been shown to be effective against many infectious organisms, including <i>P. falciparum</i>. A panel of 25 S-MGBs was synthesised, including those bearing an amidine tail group, and their antiplasmodial activity against 3D7 and Dd2 strains was determined <i>in vitro</i> using an asexual <i>P. falciparum</i> imaging assay. Determination of activity against HEK293 cells allowed for selective cytotoxicity to be measured. DNA binding studies were carried out using native mass spectrometry and DNA thermal shift assays. A comparison of 3D7 (chloroquine sensitive) and Dd2 (chloroquine resistant) potency showed no evidence of cross-resistance across the S-MGB set. <b>S-MGB-356</b>, <b>S-MGB-368</b> and <b>S-MGB-359</b>, amidine tail containing S-MGBs, were identified as the most promising hit compounds based on their selectivity indices (HEK293/3D7) of >612.6, >335.8 and >264.8, respectively. <b>S-MGB-356</b>, <b>S-MGB-368</b> and <b>S-MGB-359</b> were confirmed to bind to DNA as dimers, with gDNA thermal shifts (Δ<i>T</i> _m) of 12 °C, 3 °C and 16 °C, respectively. Together, these data demonstrate that amidine tail bearing S-MGBs are promising hit compounds against <i>P. falciparum</i>, and can be further optimised into lead compounds.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11528320/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142568566","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}