Article
Biochemistry & Molecular Biology
Tianhua Zhai, Fangyuan Zhang, Shozeb Haider, Daniel Kraut, Zuyi Huang
Summary: This study developed a computational docking approach to identify potential small-molecule inhibitors for SARS-CoV-2 3CLpro, resulting in the identification of 288 hits. Among these hits, 71 potential inhibitors of 3CLpro were further evaluated and two chemicals were found to effectively inhibit the virus with IC50 values of 19 +/- 3 mu M and 38 +/- 3 mu M, respectively. These findings, along with the developed QSAR model, can accelerate the discovery of inhibitors for related coronaviruses.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2021)
Review
Pharmacology & Pharmacy
Anirban Mandal, Ajeet Kumar Jha, Banasri Hazra
Summary: The ongoing COVID-19 pandemic poses a significant global health security threat with no specific treatment available. Research has shown that compounds from medicinal plants exhibit strong activity in inhibiting coronavirus 3CL protease, offering potential for the development of new drugs against COVID-19.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Lucile Brier, Haitham Hassan, Xavier Hanoulle, Valerie Landry, Danai Moschidi, Lowiese Desmarets, Yves Rouille, Julie Dumont, Adrien Herledan, Sandrine Warenghem, Catherine Piveteau, Paul Carr, Sarah Ikherbane, Francois-Xavier Cantrelle, Elian Dupre, Jean Dubuisson, Sandrine Belouzard, Florence Leroux, Benoit Deprez, Julie Charton
Summary: Since the end of 2019, the global outbreak of the coronavirus SARS-CoV-2 has caused a significant increase in infections and deaths worldwide. Researchers have identified two proteases, 3CLpro and papain-like protease, encoded by the virus that play a crucial role in the virus lifecycle. Targeting the 3CLpro, which is highly conserved within this viral family, a screening of over 89,000 small molecules led to the discovery of a potent inhibitor of the SARS-CoV-2 3CLpro. The mechanism of inhibition, interaction with the protease, specificity against host proteases, and promising antiviral properties in cells are reported.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Carla Di Chio, Santo Previti, Giorgio Amendola, Rahul Ravichandran, Annika Wagner, Sandro Cosconati, Ute A. Hellmich, Tanja Schirmeister, Maria Zappala, Roberta Ettari
Summary: In this study, a new series of dipeptide nitriles were developed as reversible rhodesain inhibitors at a nanomolar level. These compounds were shown to directly bind to the active site of rhodesain and act as competitive inhibitors. The most promising compounds exhibited high binding affinity and good antiparasitic activity, making them potential lead compounds for the discovery of new drugs to treat Human African Trypanosomiasis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Mengwei Zhu, Tiantian Fu, Mengyuan You, Junyuan Cao, Hanxi Yang, Xinyao Chen, Qiumeng Zhang, Yechun Xu, Xiangrui Jiang, Leike Zhang, Haixia Su, Yan Zhang, Jingshan Shen
Summary: A series of new peptidomimetic SARS-CoV-2 3CL protease inhibitors with unique P2 and P4 positions were synthesized and evaluated. Compound 1a and 2b exhibited significant 3CLpro inhibitory activities with IC50 values of 18.06 nM and 22.42 nM, respectively. Both 1a and 2b showed excellent in vitro antiviral activities against SARS-CoV-2, with EC50 values of 313.0 nM and 170.2 nM, respectively, which were 2- and 4-fold better than nirmatrelvir. Furthermore, these compounds demonstrated no significant cytotoxicity in vitro. Metabolic stability tests and pharmacokinetic studies revealed improved metabolic stability of 1a and 2b in liver microsomes, and 2b showed similar pharmacokinetic parameters to nirmatrelvir in mice.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Marko Jukic, Katarina Kores, Dusanka Janezic, Urban Bren
Summary: COVID-19, caused by SARS-CoV-2, has led to a global health crisis with millions of deaths. Limited therapeutic options prompt the need for drug repurposing to combat the disease effectively.
FRONTIERS IN CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Jiajie Zhu, Haiyan Zhang, Qinghong Lin, Jingting Lyu, Lu Lu, Hanxi Chen, Xuning Zhang, Yanjun Zhang, Keda Chen
Summary: This paper discusses the progress of peptidomimetic inhibitors targeting SARS-CoV-2 3CLpro and briefly discusses the effects of small-molecule compounds with antiviral and anti-inflammatory properties on 3CLpro.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Article
Biochemistry & Molecular Biology
Yea-In Park, Jang Hoon Kim, Siyun Lee, Ik Soo Lee, Junsoo Park
Summary: The COVID-19 pandemic has caused over six million deaths worldwide since 2019. In this study, researchers isolated eupatin from Inula japonica flowers and demonstrated its ability to inhibit coronavirus protease activity and viral replication. The results suggest that eupatin could be a potential treatment for coronavirus.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Xiaoxin Chen, Peng Li, Jianzhou Huang, Yaxun Yang, Haoyu Zhang, Zheng Wang, Zhenzhen Zhu, Jingjing Wang, Jianchen Zhang, Kevin Chen, Haiying He, Chaofeng Long, Shuhui Chen
Summary: The outbreak of SARS-CoV-2 has caused a global health and economic crisis. The use of Paxlovid requires specialized assessment of the multiple drug-drug interaction risk associated with ritonavir. We report a multiple-round SAR study that introduces a novel bicyclic [3.3.0]proline peptidyl a-ketoamide compound 4a, which exhibits excellent antiviral activities and pharmacokinetic properties. In vivo experiments using an HCoV-OC43 neonatal mice model demonstrate the good efficacy of compound 4a. Based on these findings, further SAR optimization is warranted to develop compounds with improved pharmacokinetic properties and ultimately achieve single agent efficacy in humans.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Physical
Shipra Bhati, Vikas Kaushik, Joginder Singh
Summary: This study designed a series of inhibitors targeting SARS-CoV 3CL protease with potential anti-COVID-19 infection effects.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
Wei-Chung Chiou, Meng-Shiuan Hsu, Yun-Ti Chen, Jinn-Moon Yang, Yeou-Guang Tsay, Hsiu-Chen Huang, Cheng Huang
Summary: Researchers have identified several FDA-approved drugs that can effectively inhibit the proteolytic activity of SARS-CoV-2 virus, demonstrating their therapeutic potential for treating COVID-19 and other Betacoronavirus infections.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Bibhudutta Mishra, Pranav Ballaney, Gourav Saha, Akshay Shinde, Subhadeep Banerjee, Venkatesan S. Thimmakondu, Raviprasad Aduri
Summary: Coronavirus disease 19 (COVID-19) is caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). The search for potential drug candidates to combat the virus is crucial due to the lack of vaccine or specific antiviral treatments. Through molecular docking studies, researchers have identified potential drugs that can target an essential non-structural protein of SARS-CoV-2. Further analysis and simulations have led to the identification of three molecules with high potential to be explored as drug candidates.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Engineering, Environmental
Ella Borberg, Sofiya Pashko, Fernando Patolsky
Summary: This study presents an antibody-free smart pH paper-based detection platform for rapid detection of SARS-CoV-2 infection. The platform shows ultrafast detection, simplicity, cost-efficiency, and potential for multiplexed detection of other viral infections. It has implications for worldwide mass screening, particularly in remote and developing areas.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Biochemistry & Molecular Biology
Seri Jo, Luca Signorile, Suwon Kim, Mi-Sun Kim, Oscar Huertas, Raul Insa, Nuria Reig, Dong Hae Shin
Summary: In this study, researchers identified three compounds through drug repurposing that showed strong inhibitory activity against the main protease of the novel coronavirus. One of these compounds demonstrated potential antiviral activity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Andrea Citarella, Angela Scala, Anna Piperno, Nicola Micale
Summary: The uncontrolled spread of COVID-19 caused by SARS-CoV-2 in 2020-2021 had devastating impacts on health, economy, and daily life globally. Despite approved vaccines, their long-term efficacy and safety are debated, prompting the search for new target-based drugs. Strategies targeting the coronavirus's main protease, M-pro, show promise for anti-coronavirus drug development.
Article
Chemistry, Multidisciplinary
Chihiro Uchiyama, Akane Fukuda, Minagi Mukaiyama, Yoshiki Nakazawa, Yuka Kuramochi, Kyohei Muguruma, Mitsue Arimoto, Akihiro Ninomiya, Koichiro Kako, Yohei Katsuyama, Sho Konno, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yoko Nagumo, Takeo Usui, Yoshio Hayashi
Summary: The structure of natural cyclic depsipeptide MA026 was revised through physicochemical analysis and total solid-phase synthesis, showing similar biological activity as the natural one. This revised structure has potential implications for the synthesis and application of MA026.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Medicinal
Sho Konno, Kiyotaka Kobayashi, Miki Senda, Yuta Funai, Yuta Seki, Ikumi Tamai, Laura Schaekel, Kyousuke Sakata, Thanigaimalai Pillaiyar, Akihiro Taguchi, Atsuhiko Taniguchi, Michael Guetschow, Christa E. Mueller, Koh Takeuchi, Mikako Hirohama, Atsushi Kawaguchi, Masaki Kojima, Toshiya Senda, Yoshiyuki Shirasaka, Wataru Kamitani, Yoshio Hayashi
Summary: This study reports the discovery of peptidomimetic compounds that exhibit potent activity against SARS-CoV-2 3CL protease. The most effective inhibitor, YH-53, was found to block virus replication. Structural analysis and additional experimental studies suggest that YH-53 has the potential to be a leading candidate for treating COVID-19.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Thanigaimalai Pillaiyar, Stefan Laufer
Summary: This article highlights the kinases associated with coronavirus infections and their inhibitors with antiviral and potentially anti-inflammatory, cytokine-suppressive, or antifibrotic activity.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Manoj Manickam, Sangeetha Meenakshisundaram, Thanigaimalai Pillaiyar
Summary: Studies suggest that using sEH inhibitors can increase levels of epoxy fatty acids, reduce lung inflammation, improve lung function, and may be an effective approach for the treatment of COVID-19.
ARCHIV DER PHARMAZIE
(2022)
Article
Chemistry, Medicinal
Thanigaimalai Pillaiyar, Francesca Rosato, Monika Wozniak, Jeremy Blavier, Maelle Charles, Celine Laschet, Thales Kronenberger, Christa E. Mueller, Julien Hanson
Summary: This study identified a selective GPR27 agonist and a series of new derivatives and analogs, including potent agonists with higher efficacies than the lead compound. Docking studies predicted the putative binding site and interactions of an agonist with GPR27, providing important new tools for further characterizing the (patho)physiological roles of GPR27.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Max Braune, Nico Scherf, Claudia Heine, Katja Sygnecka, Thanigaimalai Pillaiyar, Chiara Parravicini, Bernd Heimrich, Maria P. Abbracchio, Christa E. Mueller, Heike Franke
Summary: The study identified MTK as a stimulator of neurite outgrowth, mediating its effects through GPR17. The combination of MTK with GPR17 agonist significantly inhibited neuronal growth, while MTK alone showed growth-promoting effects comparable with GDNF.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Philipp Flury, Olga Eppler, Dieter Schollmeyer, Stefan Laufer, Thanigaimalai Pillaiyar
Summary: A new alkyne hydroarylation protocol for the synthesis of 3-(indol-3-yl)-3-(trifluoromethyl)acrylic acid esters was developed. The reaction of indole derivatives with ethyl/methyl 4,4,4-trifluoro-3-(indol-3-yl)but-2-enoates in trifluoroethanol showed high yields, broad substrate scope, and atom economy. The potential application of this method was demonstrated by the synthesis of CF3-substituted synthons and a new class of (un)symmetrical 3,3'-diindolylmethanes with a quaternary carbon core.
ARCHIV DER PHARMAZIE
(2022)
Review
Chemistry, Medicinal
Alp Bayrak, Julien Hanson, Stefan Laufer, Thanigaimalai Pillaiyar
Summary: In recent years, the super-conserved receptors GPR27, GPR85, and GPR173 expressed in the brain have gained significant attention in the field of medicinal science. Their functions in the body and potential in drug development have been investigated. GPR27 has been found to be important for diabetes treatment, while GPR85 is linked to brain diseases such as schizophrenia and autism. GPR173 is associated with various illnesses. The SREB family, consisting of these receptors, is highly conserved in vertebrates and predominantly expressed in the central nervous system, playing important roles in different diseases.
FUTURE MEDICINAL CHEMISTRY
(2022)
Article
Cell Biology
Dorian Dolanc, Tomaz M. Zorec, Zala Smole, Anja Maver, Anemari Horvat, Thanigaimalai Pillaiyar, Sasa Trkov Bobnar, Nina Vardjan, Marko Kreft, Helena Haque Chowdhury, Robert Zorec
Summary: This study investigated the unknown functions of GPR27, an orphan GPCR. The results showed that stimulation of GPR27 enhances aerobic glycolysis and L-lactate production in cells.
Article
Chemistry, Medicinal
Minagi Mukaiyama, Chihiro Uchiyama, Akane Fukuda, Yoshiki Nakazawa, Yuka Kuramochi, Yudai Shibata, Sho Konno, Kyohei Muguruma, Naohiro Matsugaki, Tomo Asari, Kazuyoshi Ogawa, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yoko Nagumo, Toshiya Senda, Yoshio Hayashi, Takeo Usui
Summary: MA026, a cyclic lipodepsipeptide, opens tight junctions by binding to claudin-1. In this study, it was found that the amino acid sequence order at Glu10-Leu11 is important for the TJ-opening activity of MA026. Additionally, the epimers at the C3 position of the N-terminal acyl tail showed decreased TJ-opening activity. The three-dimensional structure and systematic structure-activity relationship study of MA026 revealed that the hydrophobic region is crucial for its TJ-opening activity.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Sho Konno, Miyu Tanaka, Tomoe Mizuguchi, Haruka Toyokai, Akihiro Taguchi, Atsuhiko Taniguchi, Yoshio Hayashi
Summary: Natural macrocyclic peptides derived from microorganisms are important resources for new therapeutic agents and are biosynthesized by NRPS. The TE domain in NRPS is responsible for macrocyclization, and NRPS-TEs can be used as biocatalysts for preparing natural product derivatives. However, the substrate recognition and interaction during macrocyclization are still unknown. In this study, a substrate-based analog with mixed phosphonate warheads was developed to investigate the macrocyclization mediated by TE.
JOURNAL OF PEPTIDE SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Nina Geiger, Viktoria Diesendorf, Valeria Roll, Eva-Maria Koenig, Helena Obernolte, Katherina Sewald, Julian Breidenbach, Thanigaimalai Pillaiyar, Michael Guetschow, Christa E. Mueller, Jochen Bodem
Summary: Recently, we investigated novel pyridyl indole esters and peptidomimetics as potent inhibitors of SARS-CoV-2 main protease. We analyzed the impact of these compounds on viral replication and found that their effectiveness varied in different cell lines. In Huh-7 cells, the protease inhibitors suppressed viral replication by up to 5 orders of magnitude, while in Calu-3 cells, suppression by 2 orders of magnitude was achieved. Three pyridin-3-yl indole-carboxylates showed antiviral activity in all cell lines and also in human precision-cut lung slices.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Fumihiro Ishikawa, Sho Konno, Chiharu Uchida, Takehiro Suzuki, Katsuki Takashima, Naoshi Dohmae, Hideaki Kakeya, Genzoh Tanabe
Summary: The study introduces an in vivo activity-based protein profiling (ABPP) method for endogenous NRPS in bacteria, enabling visualization and tracking of their activities. This deepens our understanding of NRPS properties which cannot be addressed by conventional methods.
CELL CHEMICAL BIOLOGY
(2022)
Article
Chemistry, Organic
Fumihiro Ishikawa, Sho Konno, Katsuki Takashima, Hideaki Kakeya, Genzoh Tanabe
Summary: The study demonstrates a novel strategy for fluorescence protein labeling and imaging in Gram-negative bacteria, using small-molecule probes targeted at specific biosynthetic enzymes. The combination with efflux pump inhibitors significantly enhances the interaction between small-molecule probes and target proteins in live bacteria.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
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)