Article
Chemistry, Organic
Shihu Qian, Yuanzheng Huang, Jiaming Li, Yanchun Zhang, Bin Zhang, Fan Jin
Summary: A novel series of indole-2-amide-derived COX-2/5-LOX dual inhibitors were designed, synthesized, and evaluated for anti-proliferative activity. Compound 7b exhibited outstanding anti-proliferative activity against A549 and HCT-116 cell lines, with attractive COX-2 and 5-LOX inhibitory activities. Further investigation confirmed that 7b could induce apoptosis of A549 cells in a dose-dependent manner.
CHINESE JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Medicine, Research & Experimental
Humera Jahan, Nimra Naz Siddiqui, Shazia Iqbal, Fatima Z. Basha, Maria Aqeel Khan, Tooba Aslam, M. Iqbal Choudhary
Summary: This study found that indole-triazole compounds 12 and 13 can attenuate AGEs-induced inflammation by suppressing the AGE-ROS-NF-K beta pathway, suggesting their potential therapeutic value in delaying the early onset of diabetic complications.
Article
Biochemistry & Molecular Biology
John N. Philoppes, Mohamed A. Abdelgawad, Mohammed A. S. Abourehab, Mohamed Sebak, Mostafa A. Darwish, Phoebe F. Lamie
Summary: Three novel series of N-methylsulfonylindole derivatives were synthesized and their different biological activities were studied. These compounds exhibited antimicrobial, antioxidant, and anti-inflammatory activities. Additionally, one of the compounds demonstrated dual COX-2/5-LOX inhibitory activity, and its cardiovascular profile was evaluated using cardiac biomarkers and histopathological study.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Amit Kumar, Mohammad Sarwar Alam, Hinna Hamid, Vaishali Chugh, Tanvi Tikla, Rajeev Kaul, Abhijeet Dhulap, Sunil K. Sharma
Summary: This study focuses on the synthesis of 26 novel compounds and their potential for treating inflammation. Two compounds were found to significantly inhibit the COX-2 enzyme, with one compound showing the best selectivity and strongest anti-inflammatory activity without causing gastric ulcers in vivo. Molecular modeling studies provided insights into the interaction between the compound and COX-2.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Medicinal
Jian Song, Yong-Feng Guan, Wen-Bo Liu, Chun-Hong Song, Xin-Yi Tian, Ting Zhu, Xiang-Jing Fu, Ying-Qiu Qi, Sai-Yang Zhang
Summary: This study designed, synthesized, and evaluated novel coumarin-indole derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. Compound MY-413 showed potent inhibitory activities against gastric cancer cells, inhibited tubulin polymerization, and MAPK signaling pathway, induced cell apoptosis and proliferation inhibition both in vitro and in vivo. In addition, MY-413 significantly inhibited tumor growth in xenograft tumor models without obvious toxicity. Overall, MY-413 is a promising lead compound for further investigation as a potential anti-gastric cancer agent.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Immunology
Aline N. Martins, Dionys de Souza Almeida, Iziara F. Florentino, Lorrane K. da Silva Moreira, Larissa C. Turones, Daniel C. Batista, Lucas S. Machado, Boniek G. Vaz, Luciano M. Liao, Gerlon de Almeida Ribeiro Oliveira, Jose Luis Rodrigues Martins, James Oluwagbamigbe Fajemiroye, Ricardo Menegatti, Elson A. Costa, Daiany P. B. da Silva
Summary: Advances have been made in the search for new multi-target modulators to control pain and inflammation. Therefore, compound LQFM202 was synthesized and evaluated for its effects on COX-1, COX-2, and 5-LOX enzymes. The results showed that LQFM202 inhibited these enzymes and had antinociceptive and anti-inflammatory effects in animal models.
INFLAMMOPHARMACOLOGY
(2023)
Article
Chemistry, Organic
Shengguo Duan, Cong Chen, Yidian Chen, Yuchen Jie, Huan Luo, Ze-Feng Xu, Bin Cheng, Chuan-Ying Li
Summary: Two reaction modes of 1-sulfonyl-1,2,3-triazoles and pyridinium 1,4-zwitterionic thiolates were described, leading to the synthesis of different derivatives. The mechanism may involve a unique sulfur migration process not reported in previous studies.
ORGANIC CHEMISTRY FRONTIERS
(2021)
Article
Biochemistry & Molecular Biology
Mostafa M. M. El-Miligy, Ahmed K. Al-Kubeisi, Mohamed G. Bekhit, Saad R. El-Zemity, Rasha A. Nassra, Aly A. Hazzaa
Summary: New thymol - 1,5-disubstitutedpyrazole hybrids were synthesized as dual COX-2/5-LOX inhibitors. Several compounds displayed inhibitory activity comparable to celecoxib and higher than quercetin, both in vitro and in vivo. Additionally, these compounds showed superior gastrointestinal safety profile.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Pavel S. Gribanov, Anna N. Philippova, Maxim A. Topchiy, Lidiya Minaeva, Andrey F. Asachenko, Sergey N. Osipov
Summary: An efficient method for accessing novel 5-(het)arylamino-1,2,3-triazole derivatives has been developed using Buchwald-Hartwig cross-coupling reaction. The most active catalyst for the process, palladium complex [(THP-Dipp)Pd(cinn)Cl] with expanded-ring N-heterocyclic carbene ligand, affords the target molecules in high yields.
Article
Biochemistry & Molecular Biology
Han Luo, Yong-Feng Lv, Hong Zhang, Jiang-Miao Hu, Hong-Mei Li, Shou-Jin Liu
Summary: A new series of mollugin-1,2,3-triazole derivatives were synthesized using a copper(I)-catalyzed Huisgen 1,3-dipolar cycloaddition reaction, and most of them demonstrated cytotoxicity on five human cancer cell lines, with compounds 14 and 17 showing significant cytotoxicity across all five cancer cell lines.
Article
Chemistry, Organic
Pavel S. Gribanov, Edita M. Atoian, Anna N. Philippova, Maxim A. Topchiy, Andrey F. Asachenko, Sergey N. Osipov
Summary: An efficient one-pot methodology has been developed for the synthesis of 5-amino-1,2,3-triazole derivatives under solvent-free conditions, using a combination of dipolar azide-nitrile cycloaddition and Dimroth rearrangement.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Organic
Shilong Wang, Yuanyuan Zhang, Guixin Liu, Hui Xu, Lijuan Song, Jinchun Chen, Jiazhu Li, Zhen Zhang
Summary: A simple and transition-metal-free strategy has been developed for constructing 5-amino-1,2,3-triazoles, enriching their molecular diversity through further functionalization. Control experiments and DFT calculations clarify the reaction mechanism, while late-stage derivatization and gram-scale synthesis demonstrate the promising utility of this methodology.
ORGANIC CHEMISTRY FRONTIERS
(2021)
Article
Chemistry, Physical
M. J. Nagesh Khadri, Hussien Ahmed Khamees, Salma Kouser, Zabiulla, Shaukath Ara Khanum
Summary: COX and 5-LOX inhibitors are considered as sustainable agents for inflammatory treatment with analgesic and anti-inflammatory effects and low gastrointestinal toxicity. A series of compounds were developed, synthesized, and evaluated for their in-vitro enzyme inhibition, analgesic and anti-inflammatory activity, and ulcerogenic effect. Compound 10b with specific substitutions showed good inhibitory potency.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Organic
Hefei Yang, Tian-Hui Xu, Shu-Ning Lu, Zhengkai Chen, Xiao-Feng Wu
Summary: A metal-, azide- and CF3-reagent free approach for the synthesis of 5-trifluoromethyl-1,2,3-triazoles via base-mediated cascade annulation of diazo compounds with trifluoroacetimidoyl chlorides has been developed. The reaction offers advantages such as readily available reagents, mild reaction conditions, a broad substrate scope, high efficiency, and promising synthetic utility. The protocol could be scaled up to the gram scale and be applied to construct the key skeleton of the analogue of LCRF-0004.
ORGANIC CHEMISTRY FRONTIERS
(2021)
Article
Chemistry, Organic
Pavel S. Silaichev, Tetyana V. Beryozkina, Vladimir Ilkin, Mikhail S. Novikov, Wim Dehaen, Vasiliy A. Bakulev
Summary: An efficient metal-free method for synthesizing 5-amino-1,2,3-triazole-4-N-sulfonyl- and arylimidamides has been developed based on a tandem process involving cycloaddition reaction and Cornforth-type rearrangement. The reaction optimization identified several factors that facilitate the reaction, including the use of a strong base and specific 3,3-diaminoacrylonitriles. The method has a broad scope and can be applied to obtain various 5-amino-1,2,3-triazole-4-carbimidamides with different substituents.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Physical
Rajarshi Nath, M. Shahar Yar, Shelly Pathania, Gourav Grover, Biplab Debnath, Md Jawaid Akhtar
Summary: A series of novel anticonvulsant compounds were designed and synthesized, with the most active compound N-(5-chlorobenzo[d]thiazol-2-yl)-2-(2,3-dioxoindolin-1-yl)acetamide (4a) showing significant anticonvulsant activity and potential pharmaceutical value. In silico studies and molecular docking were conducted to investigate the molecular interactions and drug likeness properties of the compounds.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Pharmacology & Pharmacy
Noorul Hasan, Saima Zameer, Abul Kalam Najmi, Suhel Parvez, Mohammad Shahar Yar, Mohd Akhtar
Summary: The study explored the therapeutic potential of RFM and TDF phosphodiesterase inhibitors in treating AD induced by ICV Aβ1-42 in rats. RFM and TDF were found to significantly attenuate memory deficits and neuropathological alterations induced by Aβ1-42.
PHARMACOLOGICAL REPORTS
(2021)
Article
Chemistry, Multidisciplinary
Mohammad Mustaqeem Abdullah, Nasir A. Siddiqui, Ramzi A. Mothana, Fahd A. Nasr, Adnan J. Al-Rehaily, Omer M. Almarfadi, Shahid Karim, Kashif Haider, Md Rafi Haider, M. Shahar Yar
Summary: Benzofuran is a heterocyclic scaffold found in natural products with anti-tubercular activity. A novel series of compounds containing 3-chlorobenzofuran derivatives were designed, synthesized, and screened in vitro, with compound 3b showing the strongest inhibitory potency.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Kashif Haider, Sara Rehman, Ankita Pathak, Abul K. Najmi, Mohammad S. Yar
Summary: Targeted therapy is crucial in cancer treatment, overcoming drawbacks of conventional therapy. Heterocyclic derivatives have gained attention as cytotoxic agents, with benzothiazole being explored for its therapeutic potential. Benzothiazole-based derivatives have emerged as potent inhibitors of enzymes, with some already in clinical trials. This review highlights recent advancements in benzothiazole-based derivatives as potent anticancer agents.
ARCHIV DER PHARMAZIE
(2021)
Review
Chemistry, Medicinal
Divya Sharma, Salahuddin, Vikas Sharma, Rajnish Kumar, Sagar Joshi, Sunita Kumari, Shivani Saxena, Avijit Mazumder, Mohammad Shahar Yar, Mohamed Jawed Ahsan
Summary: This paper summarizes the general synthetic methods and anticancer activity of 1,3,4-oxadiazole, discusses the different receptors on which these drugs act, and presents pharmacophore models for topoisomerase-I, histone deacetylase, and epidermal growth factor enzymes.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Organic
Devleena Tiglani, Salahuddin, Avijit Mazumder, Mohammad Shahar Yar, Rajnish Kumar, Mohamed Jawed Ahsan
Summary: Benzimidazole and quinoline are compounds with broad spectrum activities in various pharmacological fields, and their hybrid structures have shown positive results against different diseases.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Review
Pharmacology & Pharmacy
Kashif Haider, Anku Sharma, M. Shahar Yar, Prasanna Anjaneyulu Yakkala, Syed Shafi, Ahmed Kamal
Summary: This review article summarizes the developments of small molecule KRAS inhibitors as drug candidates and the rational approaches for selectively targeting KRAS signaling in mutant cancer cells. After achieving initial success in targeting the mutant KRAS G12C variants, the current challenge is to address the resistance and efficacy issues of small molecule KRAS inhibitors. In the development of KRAS targeted therapies, the design of small molecule inhibitors that can inhibit KRAS signaling and also target other signaling pathways like RAS-SOS and RAS-PI3K needs to be extensively explored.
EXPERT OPINION ON DRUG DISCOVERY
(2022)
Review
Chemistry, Medicinal
Kashif Haider, Subham Das, Alex Joseph, M. Shahar Yar
Summary: Heterocyclic compounds containing quinazoline and quinazolinone core have shown high efficacy in cancer treatment and have been widely used in clinical practice. These drugs work by different pathways to prevent the progression of cancer cells, achieving significant results.
DRUG DEVELOPMENT RESEARCH
(2022)
Review
Chemistry, Medicinal
Shaikh Yahya, Kashif Haider, Ankita Pathak, Akram Choudhary, Pooja Hooda, Mohd Shafeeq, Mohammad Shahar Yar
Summary: Heterocyclic scaffolds of natural and synthetic origin offer a wide range of pharmacological activities, including ALR2 inhibitors for the treatment of complications related to diabetes. This study summarizes the recent developments in the pharmacologically active ALR2 heterocyclic scaffold and discusses the design, structure-activity relationships, and biological studies of these molecules.
ARCHIV DER PHARMAZIE
(2022)
Review
Chemistry, Organic
Abhishek Shankar Sharma, Salahuddin, Avijit Mazumder, Rajnish Kumar, Vimal Datt, Km Shabana, Sonakshi Tyagi, Mohammad Shahar Yar, Mohamed Jawed Ahsan
Summary: Due to their diverse applications, quinoline and 1,3,4-oxadiazole have become important heterocyclic compounds in industrial and synthetic organic chemistry. They have shown potential in various medical conditions and synthetic protocols have been developed to explore their structure-activity relationship for further research.
CURRENT ORGANIC SYNTHESIS
(2023)
Review
Biochemistry & Molecular Biology
Vikas Pradhan, Salahuddin Salahuddin, Rajnish Kumar, Avijit Mazumder, Mohammad Mustaqeem Abdullah, Mohammad Shahar Yar, Mohamed Jawed Ahsan, Zabih Ullah
Summary: Cancer is a leading cause of death worldwide, posing substantial risks to society and individuals. Despite advances in cancer prevention, therapy remains challenging. Therefore, continuous research is being conducted to search for novel anticancer agents with broader cytotoxicity range. Quinoline derivatives, which are double ring structures of the heterocyclic aromatic nitrogen molecule formed by the fusion of a benzene ring and a pyridine ring at two carbon atoms close to each other, have been found to possess a wide range of pharmacological activities, including anticancer properties. Many quinoline derivatives are available as anticancer drugs, targeting various molecular mechanisms such as topoisomerase inhibition, tyrosine kinases inhibition, heat shock protein 90 (Hsp90) inhibition, histone deacetylases (HDACs) inhibition, cell cycle arrest and apoptosis inhibition, and tubulin polymerization inhibition.
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Review
Chemistry, Medicinal
Vivek K. Gour, Shaikh Yahya, Mohammad Shahar Yar
Summary: Oxadiazoles and thiadiazoles have versatile biological applications and stability, making them potential candidates for the development of new drugs.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Multidisciplinary
Guruswamy Vaddamanu, Anandarup Goswami, Ravi Shekar Reddy Nandipati, Yamini Tanuja Malireddy, Vinod Kumar Reddy Katam Reddy, Naveen Mulakayala
Summary: Venetoclax, a drug used for treating blood cancers, produces two potential impurities during oxidative stress degradation that have similar molecular weights. These impurities could serve as reference standards in the manufacturing process of Venetoclax.
Article
Chemistry, Organic
Ajay Kumar, Salahuddin, Avijit Mazumder, Rajnish Kumar, Rakesh Sahu, Shivali Mishral, Chanchal Singh, Mohammad Shahar Yar, Mohamed Jawed Ahsan
Summary: The study synthesized and evaluated a series of quinoline derivatives with promising anti-diabetic potentials, especially compound 4e and 4d showing excellent activity. These compounds exhibited better activity compared to the standard drug pioglitazone, indicating the potential for developing new and more effective anti-diabetic agents.
INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Ravi Kumar Sadineni, Rajesh Kumar Rapolu, V. V. N. K. V. Prasada Raju, N. Srinivasu, Sireesha Malladi, Naveen Mulakayala
Summary: The compound 4-nitrophenyl cyclopropylcarbamate was used as a novel synthon for the synthesis of the anticancer drug lenvatinib, with good yields. In addition to lenvatinib, citrate, phosphate, malate, and oxalate salts of lenvatinib were also synthesized in good yields.
Correction
Biochemistry & Molecular Biology
Mohamed Marzouk, Shimaa M. Khalifa, Amal H. Ahmed, Ahmed M. Metwaly, Hala Sh. Mohammed, Hanan A. A. Taie
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Gerardo Andres Libreros-Zuniga, Danilo Pava e Pavao, Vinicius de Morais Barroso, Nathalya Cristina de Moraes Roso Mesquita, Saulo Fehelberg Pinto Braga, Glaucius Oliva, Rafaela Salgado Ferreira, Kelly Ishida, Marcio Vinicius Bertacine Dias
Summary: Tuberculosis is a major global cause of death, and the emergence of drug-resistant strains has increased the burden of this disease. New alternative therapies are constantly needed, and recent research has identified small molecules as potential inhibitors of Ldts in M. tuberculosis, which have antimycobacterial activity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xiao-Dong Wang, Yong-Si Liu, Ming-Hao Hu
Summary: In this study, a selffolded fluorescent probe was designed to selectively illuminate G4s by unfolding its intramolecular aggregation mediated by G4 binding. This probe showed more controllable background emission and promising ability to track G4 forming dynamics compared to previous disaggregation-induced emission (DIE) probes.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Xiang, Zhuo Yuan, Qichuan Deng, Linshen Xie, Dongke Yu, Jianyou Shi
Summary: This review provides a brief description of the diagnosis, pathogenesis, and potential therapeutic inhibitors for renal fibrosis. Currently, there are no clear therapeutic targets or drugs for renal fibrosis; however, some natural products may have potential efficacy for treating renal fibrosis.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Simone Giovannuzzi, Anna Nikitjuka, Bruna Rafaela Pereira Resende, Michael Smietana, Alessio Nocentini, Claudiu T. Supuran, Jean-Yves Winum
Summary: Boron-based compounds have been extensively studied in medicinal chemistry, playing a crucial role in designing small molecule drugs for various diseases. Boron is particularly valuable in developing inhibitors for metalloenzymes carbonic anhydrases, and it can modulate ligand recognition ability and selectivity. Recent advancements have led to the discovery of novel boron-based inhibitors that can inhibit carbonic anhydrases through a Lewis acid-base mechanism. Further research is needed to fully explore the potential of boron-based inhibitors and advance their clinical applications.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xinxin Liu, Lei Chen, Ze Chen
Summary: This study developed a nanostructured photosensitizer loaded with oxygen-throttling drug and demonstrated its enhanced cytotoxicity against tumor cells under hypoxic conditions. Animal experiments showed the enhanced tumor targeting capability of the photosensitizer and its inhibitory effect on tumor growth.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Shuai Jiang, Wen-Yan Li, Zai-Feng Yuan, Qin-Shi Zhao
Summary: This study isolated two new dimeric Lycopodium alkaloids and twelve previously undescribed Lycopodium alkaloids from Lycopodiastrum casuarinoides. The structures of these compounds were determined and their inhibitory activities on the Cav3.1 channel were evaluated.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yan Yang, Dong-Xiao Yan, Rui-Xue Rong, Bing-Ye Shi, Man Zhang, Jing Liu, Jie Xin, Tao Xu, Wen-Jie Ma, Xiao-Liu Li, Ke-Rang Wang
Summary: In this study, a series of nucleolar fluorescent probes based on naphthalimide derivatives were designed and synthesized, which could achieve clear nucleolar staining in living cells. The results showed that these probes exhibited good targeting to the cell nucleolus and could bind to RNA and enhance fluorescence. This has positive implications for the diagnosis and treatment of nucleolus-related diseases.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yongxi Dong, Fang Wang, Jinlan Wen, Yongqing Mao, Shanhui Zhang, Tiemei Long, Zhangxiang Yang, Lei Li, Jiquan Zhang, Li Dong, Gang Liu, Jianwei Xu
Summary: The hybrid molecules of Scutellarein and Tertramethylpyrazine show excellent neuroprotective and antiplatelet effects in the treatment of ischemic stroke. Compound 1e is particularly effective, enhancing cell membrane permeability and inhibiting cell uptake, as well as significantly reducing cerebral infarction volume.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Chen, Yuanyuan Ying, Jonathan Lalsiamthara, Yuheng Zhao, Saber Imani, Xin Li, Sijing Liu, Qingjing Wang
Summary: This paper examines the role and metabolic regulation of NAD+ in bacteria, highlighting its impact on physiology and virulence. It explores enzymes associated with NAD+ metabolism as potential targets for antibacterial drugs and vaccine candidates. Additionally, it scrutinizes the medical potential of NAD+ and provides insights for its application in biomedicine.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Jon Macicior, Daniel Fernandez, Silvia Ortega-Gutierrez
Summary: Hutchinson-Gilford progeria syndrome (HGPS), also known as progeria, is a rare genetic disease that causes premature aging and significantly reduces life expectancy. Currently, there is only one approved drug for treating progeria, but its efficacy is limited. Progerin levels are believed to be the most important biomarker related to disease severity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Fuko Hirano, Naoya Kondo, Yusuke Murata, Aya Sudani, Takashi Temma
Summary: Fluorinated alpha-methyl 3BPA derivatives showed improved water solubility, tumor targetability, and biodistribution compared to 3BPA and BPA, resulting in significantly improved tumor-to-normal tissue ratios.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Ying Shi, Jiaqin Tang, Shumeng Zhi, Ruiqi Jiang, Qing Huang, Lei Sun, Zhizhong Wang, Yanran Wu
Summary: Necroptosis is a type of cell death associated with various diseases. In this study, we identified a small molecule inhibitor, SY-1, that effectively blocks necroptosis by inhibiting the phosphorylation of RIP1/RIP3/MLKL pathway. SY-1 also showed protective effects against TNF-induced hypothermia and improved survival in mice with SIRS. These findings highlight the potential therapeutic applications of SY-1.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Andrea Bagan, Sonia Abas, Judith Pala-Pujadas, Alba Irisarri, Christian Grinan-Ferre, Merce Pallas, Itziar Muneta-Arrate, Carolina Muguruza, Luis F. Callado, Belen Perez, Elies Molins, Jose A. Morales-Garcia, Carmen Escolano
Summary: Recent studies have identified the modulation of imidazoline I-2 receptors (I-2-IR) by selective ligands as a potential strategy for treating neurodegenerative diseases. This study reports a family of bicyclic alpha-iminophosphonates that show high affinity and selectivity for I-2-IR and demonstrates their neuroprotective and anti-inflammatory effects in in vitro and in vivo models. The findings emphasize the importance of exploring structurally novel I-2-IR ligands for therapeutic strategies in neurodegeneration.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Qiuping Xiang, Tianbang Wu, Cheng Zhang, Chao Wang, Hongrui Xu, Qingqing Hu, Jiankang Hu, Guolong Luo, Xiaoxi Zhuang, Xishan Wu, Yan Zhang, Yong Xu
Summary: This study reports the discovery of a 1-(indolizin-3-yl)ethan-1-one derivative as a potent and selective CBP bromodomain inhibitor for AML drug development.
BIOORGANIC CHEMISTRY
(2024)