Article
Chemistry, Medicinal
Xu Ling, Qing-Qing Hao, Christophe Pannecouque, Erik De Clercq, Fen-Er Chen
Summary: This paper reports a study on a novel class of HIV-1 reverse transcriptase inhibitors. By synthesizing 39 derivatives, it was found that these compounds exhibited good inhibitory activity against wild-type and resistant mutant viruses, especially the rilpivirine-associated resistant mutant E138K. Molecular docking analysis provided insights into the biological activity of these compounds and identified potential drug candidates.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Ankit Kumar Singh, Adarsh Kumar, Sahil Arora, Raj Kumar, Amita Verma, Habibullah Khalilullah, Mariusz Jaremko, Abdul-Hamid Emwas, Pradeep Kumar
Summary: This review examines the structure, replication cycle, reverse transcription, and drug targets of HIV-1. It focuses on nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs), including their mechanisms of action, FDA-approved drugs, drugs in clinical trials, resistance and adverse effects, molecular docking studies, and highly active antiretroviral therapy (HAART).
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Article
Microbiology
Ming-Tain Lai, Meizhen Feng, Min Xu, Winnie Ngo, Tracy L. Diamond, Carey Hwang, Jay A. Grobler, Daria J. Hazuda, Ernest Asante-Appiah
Summary: The combination of DOR and ISL shows a high resistance barrier against HIV-1 infection. DOR/ISL exhibits strong antiviral activity and no resistance to other drugs.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Review
Chemistry, Multidisciplinary
Ankur Kumar, Simranpreet K. Wahan, Sharma Arvind Virendra, Pooja A. Chawla
Summary: This paper discusses the control of the reverse transcriptase (RT) pathway, the role of heterocyclic compounds in inhibiting the RT pathway, and recent advances in RT inhibitors. The research in this field has provided valuable insights into mechanisms, preclinical and clinical investigations, and structural activity relationships.
Article
Biochemistry & Molecular Biology
Thomas W. Kirby, Scott A. Gabel, Eugene F. Derose, Lalith Perera, Juno M. Krahn, Lars C. Pedersen, Robert E. London
Summary: This study aims to identify small molecule ligands that can interfere with the formation of active HIV-1 reverse transcriptase (RT) by understanding its maturation process. The isolated polymerase domain p51 was utilized and ligands at subdomain interfaces were identified using computational analysis and experimental techniques, with their interactions further characterized. This study provides insight into the reverse transcription process of the virus and potential new drug targets.
Article
Plant Sciences
Ermias Mergia Terefe, Faith A. Okalebo, Solomon Derese, Joseph Muriuki, Winnie Rotich, Eduard Mas-Claret, Nicholas Sadgrove, Guillermo F. Padilla-Gonzalez, Thomas A. K. Prescott, Holly Siddique, Moses K. Langat
Summary: A rare anti-HIV crotofolane diterpenoid compound was isolated in this study, showing good anti-HIV activity and low toxicity.
JOURNAL OF NATURAL PRODUCTS
(2022)
Review
Chemistry, Medicinal
Mustapha Suleiman, Faisal A. Almalki, Taibi Ben Hadda, Sarkar M. A. Kawsar, Subhash Chander, Sankaranarayanan Murugesan, Ajmal R. Bhat, Andrey Bogoyavlenskiy, Joazaizulfazli Jamalis
Summary: HIV is a major cause of AIDS, and the current treatment using HAART has severe side effects and can lead to multidrug resistance, prompting the need for new anti-HIV agents. Natural compounds, particularly from plants, have shown similar biological and structural properties to chemically synthesised compounds, with low toxicity, fewer side effects, and affordability. Coumarin, a secondary metabolite found in plants, fungi, and bacteria, has been found to inhibit various stages of the HIV replication cycle and could serve as a promising building block for the development of potent anti-HIV agents.
Article
Biochemical Research Methods
Karina Pikalyova, Alexey Orlov, Arkadii Lin, Olga Tarasova, Marcou Gilles, Dragos Horvath, Vladimir Poroikov, Alexandre Varnek
Summary: A new methodology based on generative topographic mapping (GTM) was introduced for predicting the drug resistance of HIV strains. The approach combines high accuracy and interpretability, allowing for visualization and analysis of sequence space and treatment optimization. Several case studies demonstrate the practicality of this method.
Article
Chemistry, Medicinal
Xiangyi Jiang, Boshi Huang, Waleed A. Zalloum, Chin-Ho Chen, Xiangkai Ji, Zhen Gao, Jiaojiao Dai, Minghui Xie, Dongwei Kang, Erik De Clercq, Christophe Pannecouque, Xinyong Liu, Peng Zhan
Summary: Novel diarypyrimidine derivatives were designed based on previously reported HIV-1 NNRTIs BH-11c and XJ-10c to improve antiresistance and drug-like profiles. Compound 12g showed the highest inhibitory activity against wild-type and NNRTI-resistant HIV-1 strains, with EC50 values ranging from 0.024 to 0.0010 μM. Its improved antiresistance profile compared to ETR was explained by MD simulation study and it also showed improved water solubility and other drug-like properties. Compound 12g exhibited promising pharmacokinetics parameters and could be a potential lead compound for new antiretroviral drug development.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Ruo-Lan Zhou, Christophe Pannecouque, Erik De Clercq, Shuai Wang, Fen-Er Chen
Summary: Our recent research on developing HEPT analogs for HIV therapy has identified a potent NNRTI 3 with limited anti-resistance potency. In order to address this limitation, we explored the chemical space of the solvent-protein interface and generated a series of novel HEPT analogs. Some of these analogs showed significant improvements in anti-resistance efficacy, with compound 7g being the most promising, surpassing the activity and selectivity of compound 3 by approximately 2-fold. This study provides new guidance for the development of NNRTIs.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Giavana R. Prucha, Sean Henry, Klarissa Hollander, Zachary J. Carter, Krasimir A. Spasov, William L. Jorgensen, Karen S. Anderson
Summary: This study reports the synthesis of 34 compounds that covalently inhibit reverse transcriptase to overcome the issue of resistance to non-nucleoside reverse transcriptase inhibitors. Two of these inhibitors demonstrate biochemical, structural, enzyme kinetic, mass spectrometry, and antiviral activity against HIV-1.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Plant Sciences
Carlos de Tomas, Carlos M. Vicient
Summary: Endogenous pararetroviruses (EPRVs), derived from DNA viruses of the family Caulimoviridae, are viral sequences integrated into plant genomes. This study analyzed a large number of plant genome sequences and identified 57 clusters and 13 genera of EPRVs, including a newly proposed genus called Wendovirus. There are significant differences in the abundance and distribution of EPRVs between different plant families and genera, with florendoviruses being the most abundant and widespread.
FRONTIERS IN PLANT SCIENCE
(2022)
Review
Chemistry, Medicinal
Lina Zhang, Fenju Wei, Jiwei Zhang, Chuanfeng Liu, Nerea Lopez-Carrobles, Xinyong Liu, Luis Menendez-Arias, Peng Zhan
Summary: This paper reviews the current status of HIV-1 RNase H inhibitors and discusses the problems encountered in their characterization and further development, providing an update on recent progress in the field.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Yuki Yoshida, Masakazu Honma, Yasuaki Kimura, Hiroshi Abe
Summary: Despite the availability of various anti-HIV drugs, NRTIs remain widely used and of interest. However, HIV has developed resistance against NRTIs, necessitating the search for novel therapies to combat the virus.
Article
Biochemistry & Molecular Biology
Javier Martinez del Rio, Nerea Lopez-Carrobles, Jesus I. Mendieta-Moreno, Oscar Herrera-Chacon, Adrian Sanchez-Ibanez, Jesus Mendieta, Luis Menendez-Arias
Summary: The combination of PCR and RTs has been widely used in RNA detection and gene expression analysis. Improving thermostability and nucleic acid binding affinity of RTs is crucial for enhancing the efficiency of these applications. This study investigated the effects of amino acid substitutions in the RT RNase H domain on its properties. It was found that specific substitutions resulted in loss of activity and mutations that improved cDNA synthesis efficiency also affected RNase H activity. This discovery provides evidence for a novel mechanism of RNase H inactivation.
JOURNAL OF MOLECULAR BIOLOGY
(2023)
Article
Microbiology
M. Van den Kerkhof, D. Mabille, S. Hendrickx, P. Leprohon, C. E. Mowbray, S. Braillard, M. Ouellette, L. Maes, G. Caljon
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2020)
Article
Infectious Diseases
Rafael Augusto Alves Ferreira, Celso de Oliveira Rezende Junior, Pablo David Grigol Martinez, Paul John Koovits, Bruna Miranda Soares, Leonardo L. G. Ferreira, Simone Michelan-Duarte, Rafael Consolin Chelucci, Adriano D. Andricopulo, Mariana K. Galuppo, Silvia R. B. Uliana, An Matheeussen, Guy Caljon, Louis Maes, Simon Campbell, Jadel M. Kratz, Charles E. Mowbray, Luiz Carlos Dias
Summary: Leishmaniasis is a neglected tropical disease that affects millions of people worldwide. The current drugs for treating this disease have drawbacks such as toxicity and long treatment regimens. Research has identified a promising target molecule, but in vivo tests showed poor efficacy.
PLOS NEGLECTED TROPICAL DISEASES
(2021)
Article
Pharmacology & Pharmacy
Katrien Van Bocxlaer, Kerri-Nicola McArthur, Andy Harris, Mo Alavijeh, Stephanie Braillard, Charles E. Mowbray, Simon L. Croft
Summary: In cutaneous leishmaniasis, using film-forming systems for drug delivery shows potential advantages in reducing adverse effects and improving treatment adherence. However, the efficacy of specific compounds like DNDI-0690 using this system requires further investigation and consideration.
Article
Microbiology
Magali Van den Kerkhof, Philippe Leprohon, Dorien Mabille, Sarah Hendrickx, Lindsay B. Tulloch, Richard J. Wall, Susan Wyllie, Eric Chatelain, Charles E. Mowbray, Stephanie Braillard, Marc Ouellette, Louis Maes, Guy Caljon
Summary: Oxaboroles, a novel class of antileishmanial drugs, have not shown readily emergent resistance and hold promise for future treatment. The combination of a genome-wide cosmid library and next-generation sequencing can identify resistance determinants and potential targets.
Article
Chemistry, Medicinal
Charles E. Mowbray, Stephanie Braillard, Paul A. Glossop, Gavin A. Whitlock, Robert T. Jacobs, Jason Speake, Bharathi Pandi, Bakela Nare, Louis Maes, Vanessa Yardley, Yvonne Freund, Richard J. Wall, Sandra Carvalho, Davide Bello, Magali Van den Kerkhof, Guy Caljon, Ian H. Gilbert, Victoriano Corpas-Lopez, Iva Lukac, Stephen Patterson, Fabio Zuccotto, Susan Wyllie
Summary: A compound with potential therapeutic effects on visceral leishmaniasis has been discovered and optimized to become a potential clinical candidate. This compound has shown strong anti-leishmanial activity in both in vitro and in vivo studies.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Rana Abdelnabi, Caroline S. Foo, Dirk Jochmans, Laura Vangeel, Steven De Jonghe, Patrick Augustijns, Raf Mols, Birgit Weynand, Thanaporn Wattanakul, Richard M. Hoglund, Joel Tarning, Charles E. Mowbray, Peter Sjo, Fanny Escudie, Ivan Scandale, Eric Chatelain, Johan Neyts
Summary: There is an urgent need for potent and selective antivirals against SARS-CoV-2. Pfizer has developed PF-07321332 (PF-332), a powerful inhibitor of the viral main protease (Mpro, 3CLpro), which can be taken orally and is currently in clinical development. In this study, it was found that PF-332 has equal in vitro activity against the four SARS-CoV-2 variants of concern and can completely halt replication of the alpha variant in human airway epithelial cells. The treatment with PF-332 protected Syrian Golden hamsters against infection with the beta and delta variants and prevented transmission of the SARS-CoV-2 (B.1.617.2) variant to untreated co-housed sentinels.
NATURE COMMUNICATIONS
(2022)
Article
Chemistry, Medicinal
Kirandeep Samby, Dominique Besson, Anirban Dutta, Buddhadev Patra, Angelique Doy, Paul Glossop, James Mills, Gavin Whitlock, Rob Hooft van Huijsduijnen, Alessandra Monaco, Graeme Bilbe, Charles Mowbray, Benjamin Perry, Anna Adam, Timothy N. C. Wells, Paul A. Willis
Summary: The Covid-19 pandemic has highlighted the importance of investing in the search for new medicines to address emerging health threats. Researchers have assembled the Pandemic Response Box, a collection of 400 compounds, to facilitate drug discovery in emerging infectious diseases.
ACS INFECTIOUS DISEASES
(2022)
Article
Pharmacology & Pharmacy
Tatsuro Kuzuki, Benjamin Perry, Charles Mowbray
Summary: The Neglected Tropical Disease (NTD) Drug Discovery Booster is a collaborative project that aims to develop new starting points for neglected tropical diseases through the sharing of experience and chemical libraries with pharmaceutical partners across the globe. Since 2015, the Booster has explored over 20 new starting points, converting more than half of them into new series for further development. The most advanced project is expected to deliver a preclinical candidate for leishmaniasis within the next 2 years.
YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN
(2022)
Article
Medicine, General & Internal
Jean-Selim Driouch, Maxime Cochin, Franck Touret, Paul-Remi Petit, Magali Gilles, Gregory Moureau, Karine Bathelemy, Caroline Laprie, Thanaporn Wattanakul, Palang Chotsiri, Richard M. Hoglund, Joel Tarning, Laurent Fraisse, Peter Sjo, Charles E. Mowbray, Fanny Escudie, Ivan Scnadale, Eric Chatelain, Xavier de Lamballerie, Caroline Solas, Antonine Nougairede
Summary: This study evaluated the preclinical activity of nitazoxanide against SARS-CoV-2. The results showed that nitazoxanide had some inhibitory effects on SARS-CoV-2 in vitro and in models, but the concentrations used in actual treatment were insufficient to affect viral replication in affected organs.
Article
Microbiology
Frauke Assmus, Jean-Selim Driouich, Rana Abdelnabi, Laura Vangeel, Franck Touret, Ayorinde Adehin, Palang Chotsiri, Maxime Cochin, Caroline S. Foo, Dirk Jochmans, Seungtaek Kim, Lea Luciani, Gregory Moureau, Soonju Park, Paul-Remi Petit, David Shum, Thanaporn Wattanakul, Birgit Weynand, Laurent Fraisse, Jean-Robert Ioset, Charles E. Mowbray, Andrew Owen, Richard M. Hoglund, Joel Tarning, Xavier de Lamballerie, Antoine Nougairede, Johan Neyts, Peter Sjo, Fanny Escudie, Ivan Scandale, Eric Chatelain
Summary: In the absence of drugs to treat or prevent COVID-19, drug repurposing can be a valuable strategy. However, the lack of clear translational processes and adequate preclinical profiling has hindered the success of repurposed drugs. This study proposes a systematic approach to urgent antiviral drug development, utilizing in vitro, ex vivo, and in vivo models along with pharmacokinetic modeling and simulations. The importance of assessing in vitro and in vivo potency and utilizing pharmacokinetic modeling for compound prioritization is emphasized. A standardized translational drug development platform is advocated to generate preclinical evidence for clinical trials in the context of mild-to-moderate COVID-19.
Article
Chemistry, Medicinal
Celso de Oliveira Rezende Jr, Pablo David Grigol Martinez, Rafael Augusto Alves Ferreira, Paul John Koovits, Bruna Miranda Soares, Leonardo L. G. Ferreira, Simone Michelan-Duarte, Rafael Consolin Chelucci, Adriano D. Andricopulo, An Matheeussen, Natascha Van Pelt, Guy Caljon, Louis Maes, Simon Campbell, Jadel M. Kratz, Charles E. Mowbray, Luiz Carlos Dias
Summary: This study describes the optimization of a 2-aminobenzimidazole hit for the treatment of Chagas disease, focusing on improving potency, selectivity, stability, and lipophilicity. Although the properties of the initial hits were improved, their low solubility and cytotoxicity prevented further efficacy studies in a mouse model of Chagas disease.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Taisuke Tawaraishi, Atsuko Ochida, Yuichiro Akao, Sachiko Itono, Masahiro Kamaura, Thamina Akther, Mitsuyuki Shimada, Stacie Canan, Sanjoy Chowdhury, Yafeng Cao, Kevin Condroski, Ola Engkvist, Amanda Francisco, Sunil Ghosh, Rina Kaki, John M. Kelly, Chiaki Kimura, Thierry Kogej, Kazuya Nagaoka, Akira Naito, Garry Pairaudeau, Constantin Radu, Ieuan Roberts, David Shum, Nao-aki Watanabe, Huanxu Xie, Shuji Yonezawa, Osamu Yoshida, Ryu Yoshida, Charles Mowbray, Benjamin Perry
Summary: Probing multiple proprietary pharmaceutical libraries in parallel through virtual screening led to the rapid expansion of structure-activity relationship (SAR) around hit compounds with moderate efficacy against Trypanosoma cruzi. The SAR was further developed through a potency-improving scaffold hop and design guided by phenotypic virtual screening, resulting in the identification of two promising hit compounds 54 and 85. Compound 85 showed a significant reduction in parasitemia in an in vivo model, confirming its potential as an anti-trypanosome treatment.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Shikhar Sharma, Chi-Yeh Chung, Sean Uryu, Jelena Petrovic, Joan Cao, Amanda Rickard, Nataliya Nady, Samantha Greasley, Eric Johnson, Oleg Brodsky, Showkhin Khan, Hui Wang, Zhenxiong Wang, Yong Zhang, Konstantinos Tsaparikos, Lei Chen, Anthony Mazurek, John Lapek, Pei-Pei Kung, Scott Sutton, Paul F. Richardson, Eric C. Greenwald, Shinji Yamazaki, Rhys Jones, Karen A. Maegley, Patrick Bingham, Hieu Lam, Alexandra E. Stupple, Aileen Kamal, Anderly Chueh, Anthony Cuzzupe, Benjamin J. Morrow, Bin Ren, Catalina Carrasco-Pozo, Chin Wee Tan, Dharmesh D. Bhuva, Elizabeth Allan, Elliot Surgenor, Francois Vaillant, Havva Pehlivanoglu, Hendrik Falk, James R. Whittle, Janet Newman, Joseph Cursons, Judy P. Doherty, Karen L. White, Laura Macpherson, Mark Devlin, Matthew L. Dennis, Meghan K. Hattarki, Melanie De Silva, Michelle A. Camerino, Miriam S. Butler, Olan Dolezal, Patricia Pilling, Richard Foitzik, Paul A. Stupple, H. Rachel Lagiakos, Scott R. Walker, Soroor Hediyeh-Zadeh, Stewart Nuttall, Sukhdeep Spall, Susan A. Charman, Theresa Connor, Thomas S. Peat, Vicky M. Avery, Ylva E. Bozikis, Yuqing Yang, Ming Zhang, Brendon J. Monahan, Anne K. Voss, Ian P. Street, Sarah-Jane Dawson, Mark A. Dawson, Geoffrey J. Lindeman, Melissa J. Davis, Jane E. Visvader, Thomas A. Paul
Summary: In this study, a highly potent, selective, and orally bioavailable KAT6A/KAT6B inhibitor CTx-648 was identified, which inhibits H3K23 acetylation and exhibits anti-tumor activity in ER+ breast cancer. The mechanism of action may involve the modulation of transcriptional and epigenetic profiles.
CELL CHEMICAL BIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Yuichiro Akao, Stacie Canan, Yafeng Cao, Kevin Condroski, Ola Engkvist, Sachiko Itono, Rina Kaki, Chiaki Kimura, Thierry Kogej, Kazuya Nagaoka, Akira Naito, Hiromi Nakai, Garry Pairaudeau, Constantin Radu, Ieuan Roberts, Mitsuyuki Shimada, David Shum, Nao-aki Watanabe, Huanxu Xie, Shuji Yonezawa, Osamu Yoshida, Ryu Yoshida, Charles Mowbray, Benjamin Perry
Summary: An innovative pre-competitive virtual screening collaboration was used to validate and optimize a compound for visceral leishmaniasis, expanding the chemical structure and improving activity and selectivity through structure-activity relationship analysis.
RSC MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Paul J. Koovits, Marco A. Dessoy, An Matheeussen, Louis Maes, Guy Caljon, Leonardo L. G. Ferreira, Rafael C. Chelucci, Simone Michelan-Duarte, Adriano D. Andricopulo, Simon Campbell, Jadel M. Kratz, Charles E. Mowbray, Luiz C. Dias
RSC MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
