Future medicinal chemistry最新文献_第2页

Design and application of CCR8 antagonists.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-10 DOI: 10.1080/17568919.2025.2476381

Tom Van Loy, Dominique Schols, Steven De Jonghe

引用次数: 0

Key developments in fluorinated heterocycles.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-06 DOI: 10.1080/17568919.2025.2476385

Carla Rizzo, Antonio Palumbo Piccionello

引用次数: 0

Synthesis and in vitro antitrypanosomatid activity of novel 5-nitroindole-rhodanine conjugates.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-01 Epub Date: 2025-02-24 DOI: 10.1080/17568919.2025.2470110

Emce Badenhorst, Janine Aucamp, Christina Kannigadu, Helena D Janse van Rensburg, Keisuke Suganuma, David D N'Da

{"title":"Synthesis and in vitro antitrypanosomatid activity of novel 5-nitroindole-rhodanine conjugates.","authors":"Emce Badenhorst, Janine Aucamp, Christina Kannigadu, Helena D Janse van Rensburg, Keisuke Suganuma, David D N'Da","doi":"10.1080/17568919.2025.2470110","DOIUrl":"10.1080/17568919.2025.2470110","url":null,"abstract":"Aim: Trypanosomatid diseases, leishmaniasis and trypanosomiasis are vector-borne parasitic diseases that can cause death and catastrophic economic losses for millions of people. The growing resistance of trypanosomatid parasites to current treatments highlights the urgent need for new therapeutic agents. This study explored 5-nitroindole-rhodanine conjugates to identify promising new compounds with the potential for future development as antitrypanosomatid treatments.Materials and methods: The conjugates were synthesized in a multi-step process and evaluated in vitro for antileishmanial activity against Leishmania (L.) donovani and L. major strains. Cytotoxicity was assessed on Vero and THP-1 cells. Due to the taxonomic relation to Trypanosoma spp. the compounds were also screened for in vitro activity against species that cause zoonotic trypanosomiasis.Results and conclusion: Several hits were found with leishmanicidal activity against both L. donovani and L. major strains. Of these, 3d was identified as a potential early lead that exhibited nanomolar cidal activity against L. major, and greater selectivity than the reference drug amphotericin B. However, the compounds did not have similar activity levels against Trypanosoma spp. Hence, these compounds should be further investigated for their mechanism of action and in vivo antileishmanial activity to determine their potential as a leishmaniasis treatment.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"557-573"},"PeriodicalIF":3.2,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11901381/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143491486","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

Synthesis of novel quinoline-thiazolobenzimidazolone hybrids as anticancer agents through caspase-dependent apoptosis.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-01 Epub Date: 2025-02-26 DOI: 10.1080/17568919.2025.2470112

Houria Bouria, Hayette Alliouche, Mohamed Imed Chouiter, Ali Belfaitah, Teresa Pacheco, Viktor Gala, David Pereira, Artur M S Silva

{"title":"Synthesis of novel quinoline-thiazolobenzimidazolone hybrids as anticancer agents through caspase-dependent apoptosis.","authors":"Houria Bouria, Hayette Alliouche, Mohamed Imed Chouiter, Ali Belfaitah, Teresa Pacheco, Viktor Gala, David Pereira, Artur M S Silva","doi":"10.1080/17568919.2025.2470112","DOIUrl":"10.1080/17568919.2025.2470112","url":null,"abstract":"Aim: This work explores the synthesis of new bi-heterocyclic hybrid compounds based on quinoline ring and investigates their potential as anticancer agents.Materials & methods: The novel fused quinoline-thiazolo[3,2-a] benzimidazole-3(2 h)one hybrids were prepared by regioselective nucleophilic ring opening of the corresponding quinolinyl-oxiranes. In vitro cytotoxic activity was evaluated against human lung (A549) and gastric (AGS) cancer cell lines.Results: Global results showed that all tested compounds have promising inhibitory properties. Compounds 17 and 18 bearing two methoxy groups on the quinoline ring have exhibited remarkable and interesting activities. The investigation of the cell death process showed that these compounds activated a caspase-dependent apoptosis pathway. Results were further supported by molecular docking studies.Conclusion: Both compounds exhibited good drug-like characteristics, which make them promising drug candidates.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"543-555"},"PeriodicalIF":3.2,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11901420/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143500287","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

Optimizing selective estrogen receptor degraders for anticancer drug development. 优化抗癌药物开发中的选择性雌激素受体降解剂。

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-01 Epub Date: 2025-02-26 DOI: 10.1080/17568919.2025.2467615

Neha Bhatia, Shashank Kumar, Lajya Devi Goyal, Suresh Thareja

引用次数: 0

A comprehensive review on the latest advances of dimeric anticancer prodrugs.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-01 Epub Date: 2025-02-20 DOI: 10.1080/17568919.2025.2463884

Zhila Imani, Ebrahim Saeedian Moghadam, Zahra Imani, Mohsen Amini, Fatemeh Atyabi, Rassoul Dinarvand

{"title":"A comprehensive review on the latest advances of dimeric anticancer prodrugs.","authors":"Zhila Imani, Ebrahim Saeedian Moghadam, Zahra Imani, Mohsen Amini, Fatemeh Atyabi, Rassoul Dinarvand","doi":"10.1080/17568919.2025.2463884","DOIUrl":"10.1080/17568919.2025.2463884","url":null,"abstract":"The advancement of targeted drug delivery systems has opened up a wide array of opportunities in cancer therapy, leading to the exploration of various strategies. Among these, the use of prodrugs stands out as a particularly promising approach in targeted cancer treatment, aimed at enhancing the selectivity and effectiveness of cytotoxic agents. In the last few years, there has been considerable progress in the area of dimeric-based prodrugs aimed at cancer therapy. The advantages presented by dimeric-based prodrugs have significantly improved the efficiency of delivering anticancer drugs, characterized by a high drug loading capacity, advantageous pharmacokinetics, and drug release that responds to tumor stimuli. With respect to the importance of drug dimerization in the field of prodrug development, herein we review the latest reports covering research in dimeric prodrugs. We have categorized the article according to the reported anticancer agents. We have also spent a great deal of attention on different types of used linkers and methods of the dissociation of dimeric prodrugs into free monomeric drugs. Readers will easily be able to compare between the reported research using the same drugs with different linkers or different dissociation methods as well as different cancer cell lines targeted in the studies.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"709-723"},"PeriodicalIF":3.2,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11938984/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143457537","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

A call to develop tramadol enantiomer for overcoming the tramadol crisis by reducing addiction.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-01 Epub Date: 2025-02-11 DOI: 10.1080/17568919.2025.2463314

Ilaria D'Acquarica, Israel Agranat

引用次数: 0

Protein profiling uncovers IGF-1R inhibition potential of 3-(2-furoyl)-indole scaffolds in hepatocellular carcinoma.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-01 Epub Date: 2025-03-03 DOI: 10.1080/17568919.2025.2467616

Efficiency Myrsing, H M Chandra Mouli, Pallaprolu Nikhil, Deepali, Abhishek Sahu, Anupam Jana, P Ramalingam

{"title":"Protein profiling uncovers IGF-1R inhibition potential of 3-(2-furoyl)-indole scaffolds in hepatocellular carcinoma.","authors":"Efficiency Myrsing, H M Chandra Mouli, Pallaprolu Nikhil, Deepali, Abhishek Sahu, Anupam Jana, P Ramalingam","doi":"10.1080/17568919.2025.2467616","DOIUrl":"10.1080/17568919.2025.2467616","url":null,"abstract":"Aim: This study investigates the anti-proliferative potential and possible molecular mechanisms of 3-(2-furoyl)-indole derivatives against HepG2.Method: Identified hit compounds (4a, 4b, 4c) using MTT screening, were further investigated for their efficacy and mechanism of action through FACS studies, in-silico molecular docking, molecular dynamics (MD) simulations, and label-free quantitative proteome and ADMET prediction.Results: Lead compound 4a, showed IC50 of 27 µM against HepG2 cells and a binding score of -8.077 kcal/mol against IGF-1 R (PDB ID: 5XFS) and formed a stable complex 100 ns. Proteomic study revealed significant downregulation of the IGF-1 R downstream signaling molecules and showed minimal toxicity and favorable drug-like properties.Conclusion: These findings suggest that 4a is a promising IGF-1 R inhibitor and potential drug candidate against drug resistance hepatocellular carcinoma (HCC).","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"513-528"},"PeriodicalIF":3.2,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11906113/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143540742","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

3,5-Disubstituted pyrazoline as a promising core for anticancer agents: mechanisms of action and therapeutic potentials.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-01 Epub Date: 2025-03-13 DOI: 10.1080/17568919.2025.2476393

Basma S Gabr, Abdelrahman R Shalabi, Mona F Said, Riham F George

引用次数: 0

Targeting cyclin-dependent kinase 2 (CDK2) interactions with cyclins and Speedy 1 (Spy1) for cancer and male contraception.

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-03-01 Epub Date: 2025-03-04 DOI: 10.1080/17568919.2025.2463868

Jeanine Giarolla, Kelsey A Holdaway, Maryam Nazari, Laila Aiad, Bidisha Sarkar, Gunda I Georg

引用次数: 0