Review
Biochemistry & Molecular Biology
Nilakshi Barua, Alak Kumar Buragohain
Summary: Curcumin, derived from the plant Curcuma longa, has been extensively studied for its biological and chemical properties, displaying a range of pharmacological activities such as antimicrobial, anti-inflammatory, antioxidant, and antitumor effects. Its potential in improving tuberculosis outcomes has been identified, but there is a scarcity of reviews on its antitubercular activity. Further preclinical and clinical investigations are crucial before recommending curcumin formulations for public health use against tuberculosis.
Article
Microbiology
Wang Xiang, Hualong He, Xianjie Duan, Zhiqun He, Xinyue Xu, Mengya Liao, Fei Teng, Xiao Li, Tianwen Luo, Jumei Zeng, Luoting Yu, Chao Gao
Summary: About a quarter of the world's population is infected with Mycobacterium tuberculosis. With the emergence of multidrug-resistant tuberculosis, there is an urgent need for the development of new anti-tuberculosis drugs. In this study, a series of compounds based on the indole and benzomorpholine were designed and synthesized. The preferred compound B18 showed strong antimycobacterial activity and specifically targeted DprE1. B18 is a new type of effective reversible DprE1 inhibitor.
MICROBIOLOGY SPECTRUM
(2023)
Article
Biochemistry & Molecular Biology
Estevao Silveira Grams, Alessandro Silva Ramos, Mauro Neves Muniz, Raoni S. Rambo, Marcia Alberton Perello, Nathalia Sperotto, Laura Calle Gonzalez, Lovaine Silva Duarte, Luiza Galina, Adilio Silva Dadda, Guilherme Arrache Goncalves, Cristiano Valim Bizarro, Luiz Augusto Basso, Pablo Machado
Summary: By synthesizing and evaluating a series of compounds, it was found that two of them exhibited similar antibacterial effects to isoniazid and showed no significant toxicity to host cells. The chemical stability and permeability of these compounds were also assessed.
Article
Biophysics
Sandra Montalvo-Quiros, Sergio Gomez-Grana, Maria Vallet-Regi, Rafael C. Prados-Rosales, Blanca Gonzalez, Jose L. Luque-Garcia
Summary: Tuberculosis remains a major public health issue with a lack of effective vaccine and the emergence of highly antibiotic-resistant strains of Mycobacterium tuberculosis. Silver nanoparticles show high bactericidal efficacy, but their relatively high toxicity calls for the design of nanocarriers for safe delivery. Mesoporous silica nanoparticles have been used as carriers for silver nanoparticles as antimycobacterial agents, demonstrating good capability against Mtb with different synthetic approaches.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2021)
Article
Plant Sciences
Frederikke D. Andersen, Katja D. Pedersen, Dennis Wilkens Juhl, Tobias Mygind, Paul Chopin, Esben B. Svenningsen, Thomas B. Poulsen, Marie Braad Lund, Andreas Schramm, Charlotte H. Gotfredsen, Thomas Torring
Summary: This study reveals that triculamin and alboverticillin, two natural products with potent and specific activity against mycobacteria, are actually the same lasso peptide. By determining the structure using 2D NMR spectroscopy and exploring the bioactivity, we found that their precursor peptides have a follower instead of a leader peptide, which is different from known lasso peptides.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Biochemistry & Molecular Biology
Michelle Miranda-Velez, Golam Sabbir Sarker, Priya Ramisetty, Sandra Geden, Priscila Cristina Bartolomeu Halicki, Thirunavukkarasu Annamalai, Yuk-Ching Tse-Dinh, Kyle H. Rohde, Joong Ho Moon
Summary: Mycobacterial infectious diseases, particularly tuberculosis (TB), are a significant global public health concern. Current TB drugs primarily target replicating cells and are ineffective against nonreplicating Mycobacterium tuberculosis (Mtb). This study reports the antimycobacterial effects of poly(guanylurea)-piperazine (PGU-P), which disrupts the mycobacterial membrane potential and bioenergetics. PGU-P also exhibits promising activity against pathogenic Mtb, making it a potential candidate for the development of novel antimycobacterial drugs.
Article
Chemistry, Medicinal
Daria Elzbieta Nawrot, Ghada Bouz, Ondrsi Jandourek, Klara Konecna, Pavla Paterova, Pavel Barta, Martin Novak, Radim Kucera, Julia Zemanova, Martin Forbak, Jana Kordulakova, Oto Pavlis, Pavla Kubickova, Martin Dolezal, Jan Zitko
Summary: Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is the leading cause of death among infectious diseases caused by a single microbe. With the emergence of antimicrobial resistance, the success rate of treating this infection is decreasing, and there is an urgent need for novel treatments. In this study, a novel series of compounds inspired by combining fragments from first-line and second-line agents for tuberculosis were synthesized and evaluated. Compound 10c from the second series showed selective and potent antimycobacterial activity against both drug-sensitive and drug-resistant Mtb strains, with no cytotoxicity. The compound targeted methionine metabolism rather than the folate pathway and had a long half-life, overcoming the limitations of current drugs for tuberculosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Bhaiyyasaheb Harale, Saqib Kidwai, Divya Ojha, Manisha Singh, Dwarika Kumar Chouhan, Ramandeep Singh, Vijay Khedkar, Ambadas B. Rode
Summary: Riboflavin derivatives showed promising antimycobacterial activity, with compound 5a being a lead candidate due to its potency and low toxicity. These compounds may exert their antimycobacterial effects through inhibition of riboflavin biosynthesis pathway via FMN riboswitch.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Plant Sciences
Kadidiatou O. Ndjoubi, Rajan Sharma, Jelili A. Badmus, Ayesha Jacobs, Audrey Jordaan, Jeanine Marnewick, Digby F. Warner, Ahmed A. Hussein
Summary: Plectranthus madagascariensis, a medicinal plant native to South Africa, has shown potential in the treatment of tuberculosis and psoriasis due to its bioactive compounds with antimicrobial and antioxidant properties. The phytochemical studies of this plant led to the isolation of five known royleanone abietanes, which showed promising results in inhibiting Mycobacterium tuberculosis and demonstrating comparable toxicity to tamoxifen against HaCaT cells. The plant is considered an important ethnomedicinal plant and a promising source of diterpenoids for potential therapeutic applications.
Article
Biochemistry & Molecular Biology
Meng-Yu Xia, Yu-Xiang Cai, Jun-Xian Chen, Xin Zhao, Hong-Mei Dong, Zai-Chang Yang
Summary: In this study, fifteen 1,2,4-triazole derivatives were synthesized and evaluated for their MIC values against Mycobacterium tuberculosis (Mtb), ranging from 2 to 32 μg/mL. The antimycobacterial activity of these compounds was found to be positively correlated with the KatG enzyme docking score. Compound 4 exhibited the strongest bactericidal activity with an MIC of 2 μg/mL. It also showed low toxicity to animal cells and the ability to bind firmly to the Mtb KatG active site. The study suggests that compound 4 inhibits KatG, leading to the accumulation of ROS and oxidative destruction, ultimately causing the death of Mtb.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Review
Medicine, Research & Experimental
Aditi Chauhan, Manoj Kumar, Awanish Kumar, Kajal Kanchan
Summary: Tuberculosis is one of the deadliest infectious diseases with serious global threat, as the high drug resistance of Mycobacterium tuberculosis leads to increasing number of cases each year. Available antimycobacterial drugs are classified into first line, second line, and third line antibiotics, but years of non-judicious and uncontrolled use have created the significant problem of multidrug-resistant tuberculosis (MDR). Research focuses on new drug candidates, repurposed drugs, and drug combinations for more effective treatment of MDR tuberculosis or reducing chemotherapy time for drug sensitive TB.
Article
Chemistry, Medicinal
Andre Campanico, Shrika G. Harjivan, Elisabete Freitas, Marco Serafini, M. Manuela Gaspar, Rita Capela, Pedro Gomes, Audrey Jordaan, Ana M. Madureira, Vania Andre, Andreia B. Silva, M. Teresa Duarte, Isabel Portugal, Joao Perdigao, Rui Moreira, Digby F. Warner, Francisca Lopes
Summary: This study successfully improved the metabolic stability and solubility of N-acetyl azaaurones by replacing the N-acetyl moiety with a N-carbamoyl group. The new N-carbamoyl azaaurones exhibited potent antimycobacterial activity against drug-susceptible and drug-resistant M. tuberculosis isolates, with improved microsomal stability and kinetic solubility. These findings highlight the potential of azaaurones as antimycobacterial agents.
Article
Chemistry, Organic
Xiaodong Gu, Ling Meng, Mingliang Li, Jun (Joelle) Wang
Summary: A Cu(I)/(R,R)-Ph-BPE-catalyzed enantioselective hydroamination of 2H-chromenes and 2H-thiochromenes with anthranils has been developed, allowing for efficient and atom-economical asymmetric access to a series of 4-arylamino chromanes and thiochromanes with high yields (up to 96%) and excellent enantioselectivities (up to 99% ee). These valuable chiral chromane and thiochromane products serve as key intermediates for accessing nitrogen-, oxygen- and sulfur-containing bioactive compounds with increased molecular complexity.
ORGANIC CHEMISTRY FRONTIERS
(2021)
Article
Chemistry, Medicinal
Pengxu Wang, Sarah M. Batt, Bin Wang, Lei Fu, Rongfei Qin, Yu Lu, Gang Li, Gurdyal S. Besra, Haihong Huang
Summary: In this study, a series of novel thiophene-arylamide compounds were designed and synthesized through a structure-based scaffold hopping strategy, showing potent antimycobacterial activity and low cytotoxicity. The representative compound 25a demonstrated significant bactericidal activity in an acute mouse model of tuberculosis.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Jacqueline V. Lara-Espinosa, Maria Fernanda Arce-Aceves, Manuel O. Lopez-Torres, Vasti Lozano-Ordaz, Dulce Mata-Espinosa, Jorge Barrios-Payan, Carlos Alfredo Silva-Islas, Perla D. Maldonado, Brenda Marquina-Castillo, Rogelio Hernandez-Pando
Summary: Curcumin (CUR), a natural product with antioxidant, anti-inflammatory, and antibacterial activities, has been found to have a bactericidal effect on pulmonary mycobacterial infection and reduce neuroinflammation in a model of progressive pulmonary tuberculosis in mice. This suggests that CUR has potential as an adjuvant therapy in TB treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Multidisciplinary
Eloi P. Coutant, Glwadys Gagnot, Vincent Hervin, Racha Baatallah, Sophie Goyard, Yves Jacob, Thierry Rosek, Yves L. Janin
CHEMISTRY-A EUROPEAN JOURNAL
(2020)
Article
Chemistry, Applied
M. Traversier, T. Gaslonde, M. Lecso, S. Michel, E. Delannay
INTERNATIONAL JOURNAL OF COSMETIC SCIENCE
(2020)
Article
Allergy
Sophie Goyard, Bianca Balbino, Rebecca S. Chinthrajah, Shu-Chen Lyu, Yves L. Janin, Pierre Bruhns, Pascal Poncet, Stephen J. Galli, Kari C. Nadeau, Laurent L. Reber, Thierry Rose
Article
Microbiology
Ali Tahrioui, Sergio Ortiz, Onyedikachi Cecil Azuama, Emeline Bouffartigues, Nabiha Benalia, Damien Tortuel, Olivier Maillot, Smain Chemat, Marina Kritsanida, Marc Feuilloley, Nicole Orange, Sylvie Michel, Olivier Lesouhaitier, Pierre Cornelis, Raphael Grougnet, Sabrina Boutefnouchet, Sylvie Chevalier
FRONTIERS IN MICROBIOLOGY
(2020)
Article
Chemistry, Multidisciplinary
Glwadys Gagnot, Vincent Hervin, Eloi P. Coutant, Sophie Goyard, Yves Jacob, Thierry Rose, Fatima Ezzahra Hibti, Alessia Quatela, Yves L. Janin
Summary: This work focuses on the design and synthesis of luciferin analogues related to blue-hued coelenterazine, aiming to produce photons possibly at different wavelengths. Despite the presence of substituents found in actual substrates, no bioluminescence was observed with these compounds, however, they produced light signals through chemiluminescence in a phosphate buffer. The addition of a quaternary ammonium salt in the buffer increased the light signal intensity, contributing to the determination of emission spectra of these luciferin analogues.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Immunology
Francois Anna, Sophie Goyard, Ana Ines Lalanne, Fabien Nevo, Marion Gransagne, Philippe Souque, Delphine Louis, Veronique Gillon, Isabelle Turbiez, Francois-Clement Bidard, Aline Gobillion, Alexia Savignoni, Maude Guillot-Delost, Francois Dejardin, Evelyne Dufour, Stephane Petres, Odile Richard-Le Goff, Zaineb Choucha, Olivier Helynck, Yves L. Janin, Nicolas Escriou, Pierre Charneau, Franck Perez, Thierry Rose, Olivier Lantz
Summary: This study conducted in Paris conurbation found that the prevalence of SARS-CoV-2 infection in active workers was approximately 11.6% in May-July 2020, higher than laboratory testing positivity rates. The research also indicated that some infected individuals did not exhibit systemic IgG responses, suggesting that the true infection rate may have reached 16.6%, with anosmia and ageusia being common symptoms of infection.
EUROPEAN JOURNAL OF IMMUNOLOGY
(2021)
Article
Multidisciplinary Sciences
Juliette Fernandez, Cedric Hassen-Khodja, Virginie Georget, Thierry Rose, Yves Jacob, Yves L. Janin, Sebastien Nisole, Pierre-Olivier Vidalain, Nathalie J. Arhel
Summary: The recent emergence and reemergence of viruses in the human population has emphasized the necessity of developing broader panels of therapeutic molecules. High-throughput screening assays can identify innovative antiviral molecules by providing access to untargeted steps of the viral replication cycle. The development of an innovative protein complementation assay, named alpha Centauri, allows for the measurement of viral translocation between subcellular compartments, offering a robust readout of specific steps of viral infection in a multiwell format suitable for high-throughput screening.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Chemistry, Organic
Glwadys Gagnot, Pierre Legrand, Amira Tadros, Fatima Ezzahra Hibti, Alessia Quatela, Yves L. Janin
Summary: Research on new chemiluminescent substances related to marine luciferin coelenterazine led to the synthesis of nitrogen-rich pyridopyrazine-bearing analogues, including the benzyl-bearing pyridopyrazinols. Challenges were faced in the synthesis of halogenated pyridopyrazines, with varying degrees of difficulties encountered. Despite these challenges, the target O-acetylated luciferin and its derivative were successfully prepared, with their chemiluminescence emission spectra determined.
SYNTHESIS-STUTTGART
(2021)
Article
Virology
Cyrille Mathieu, Franck Touret, Clemence Jacquemin, Yves L. Janin, Antoine Nougairede, Manon Brailly, Magalie Mazelier, Didier Decimo, Virginie Vasseur, Aymeric Hans, Jose-Carlos Valle-Casuso, Xavier de Lamballerie, Branka Horvat, Patrice Andre, Mustapha Si-Tahar, Vincent Lotteau, Pierre-Olivier Vidalain
Summary: The development of a SARS-CoV-2 infection reporting system facilitates the screening of compound libraries to discover new antiviral drugs. The study found that inhibitors of pyrimidine biosynthesis and NADPH oxidase (NOX) inhibitors have inhibitory effects on SARS-CoV-2 replication.
Article
Biochemistry & Molecular Biology
Wiem Elloumi, Amina Maalej, Sergio Ortiz, Sylvie Michel, Mohamed Chamkha, Sabrina Boutefnouchet, Sami Sayadi
Summary: This study investigated the phenolic composition of P. lentiscus L. distilled leaves and its potential against key enzymes related to skin aging. The results showed that the ethyl acetate extract of PDL contained a high amount of flavonol glycoside. Transdermal diffusion study indicated that myricetin-3-O-rhamnoside had the highest transmission rate through the skin membrane barrier. The extract, along with myricetin-3-O-rhamnoside and quercetin-3-O-rhamnoside, demonstrated significant inhibitory activities against tyrosinase and elastase enzymes, without being cytotoxic. Overall, these findings suggest that they could be effective agents for treating skin pigmentation and elasticity problems.
Article
Chemistry, Organic
Pierre Legrand, Yves L. Janin
Summary: This article reports an improved method for the synthesis of 2-hydroxypyrazines, which can enhance the regioselectivity and yield of the product. By using tetraalkylammonium hydroxide as the reaction parameter, starting from phenylglyoxal and alpha-aminoamides, pyrazine-containing new chemical entities of potential interest in medicinal chemistry were obtained.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Yves L. Janin
Summary: This perspective paper discusses the challenges medicinal chemists face in drug discovery and emphasizes the importance of academic researchers in addressing these challenges. The paper presents successful examples of drug candidate discoveries and provides suggestions for contributions from academic medicinal chemists. It highlights the need for increased funding support for academic research in drug development.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Agronomy
Nabiha Benalia, Abdenour Boumechhour, Sergio Ortiz, Cristian A. Echague, Thorsten Rose, Bernd L. Fiebich, Smain Chemat, Sylvie Michel, Brigitte Deguin, Saliha Dahamna, Sabrina Boutefnouchet
Summary: Pistacia lentiscus L. is commonly found in the Mediterranean basin, and its fruit oil has been used in traditional medicine and promoted by commercial brands. This study evaluated the safety of using Pistacia lentiscus fruit oil as a cosmetic ingredient and identified the presence of alkylsalicylic acids, which call for further quantification for potential skin irritants.
OCL-OILSEEDS AND FATS CROPS AND LIPIDS
(2021)
Article
Plant Sciences
Natthinee Anantachoke, Duangporn Lovacharaporn, Vichai Reutrakul, Sylvie Michel, Thomas Gaslonde, Pawinee Piyachaturawat, Kanoknetr Suksen, Samran Prabpai, Narong Nuntasaen
PHARMACEUTICAL BIOLOGY
(2020)
Meeting Abstract
Toxicology
Sandra Sinno-Tellier, Audrey Arnaud, Jerome Langrand, Gael Le Roux, Sylvie Michel, Luc De Haro, Nathalie Paret
CLINICAL TOXICOLOGY
(2020)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)