Review
Biochemistry & Molecular Biology
Qiuzi Dai, Qinsheng Sun, Xiaorong Ouyang, Jinyang Liu, Liye Jin, Ahao Liu, Binsheng He, Tingting Fan, Yuyang Jiang
Summary: 1,3,5-triazine derivatives, also known as s-triazines, have shown their potential as anticancer agents. Several s-triazine derivatives have been approved for the treatment of refractory ovarian cancer, metastatic breast cancer, and leukemia. This review focuses on the medicinal chemistry of s-triazines and their targeting of topoisomerases, tyrosine kinases, phosphoinositide 3-kinases, NADP+-dependent isocitrate dehydrogenases, and cyclin-dependent kinases in various signaling pathways. It provides a comprehensive summary of the discovery, structure optimization, and biological applications of these s-triazine derivatives as anticancer drugs.
Article
Multidisciplinary Sciences
Mohamed R. Elmorsy, Ehab Abdel-Latif, Hatem E. Gaffer, Samar E. Mahmoud, Ahmed A. Fadda
Summary: 3-Amino-4,6-dimethylpyrazolopyridine was used as a precursor to synthesize new pyridopyrazolo-triazine and pyridopyrazolo-triazole derivatives. The synthesized compounds were identified by spectroscopic analyses. The anticancer activity of these derivatives was investigated in different carcinoma cell lines, and some compounds showed significant activity.
SCIENTIFIC REPORTS
(2023)
Review
Chemistry, Applied
N. Jeelan Basha, S. M. Basavarajaiah, Swathi Baskaran, Prasanna Kumar
Summary: This article introduces the diverse biological activities of the naturally occurring bioactive molecule embelin and its derivatives, including anticancer and antimalarial activities. Through structural activity relationship and docking studies, target-specific activities of these molecules have been identified. Recent research indicates that embelin and its derivatives possess a broad spectrum of medicinal properties.
NATURAL PRODUCT RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Heba M. Refaat, Atallh A. M. Alotaibi, Necmi Dege, Ayman El-Faham, Saied M. Soliman
Summary: In this study, two new Zn(II) complexes were synthesized using the BPMT ligand and their structures were confirmed by X-ray diffraction. These complexes showed significant antibacterial, antioxidant, and anticancer activities, demonstrating interesting biological properties.
Article
Biochemistry & Molecular Biology
Uchechukwu Susan Oruma, Pius Oziri Ukoha, Chiamaka Peace Uzoewulu, Joseph Chinedum Ndefo, Sabastine Chinweike Ugwuoke, Nkechinyere Nwanneka Ukwueze, Tochukwu Emmanuella Eze, Lilian Chinenye Ekowo, Florence Uchenna Eze, Uchenna Vivian Chinaegbomkpa, Sunday Nwankwo Okafor, Chigozie Julius Ezeorah
Summary: The tripodal Schiff base ligand, MT, and its trinuclear Dy(III), Er(III), and Gd(III) complexes were synthesized and characterized. The ligand is hexadentate and coordinates to the Ln(III) ions through the oxygen atoms of the carboxylic group. The trinuclear complexes exhibit potential biological activity, with MT showing higher activity against micro-organisms and a wide range of effective doses. In vivo antimalarial studies suggest that MT could serve as an effective antimalarial agent. Molecular docking simulation studies showed that the Er(III)MT complexes have the ability to inhibit SARS-CoV-2 and E. coli DNA gyrase through effective binding interactions.
Article
Environmental Sciences
D. Ravichandran, R. Akilan, S. Vinnarasi, R. Shankar, S. K. Khadheer Pasha, Sivakumar Manickam
Summary: Modifying structures and doping in g-C3N4 quantum dots have been proven effective in tuning their properties. Functionalizing tri-s-triazine and tri-nitro tri-s-triazine structures with hydrogen improves their planarity and reactivity, with additional B doping further enhancing these properties. The study suggests that highly reactive sheets can potentially be used for removing hazardous ions and molecules from industrial waste.
Review
Chemistry, Medicinal
Zefeng Zhao, Meng Nian, Haifa Qiao, Xiaohang Yang, Shaoping Wu, Xiaohui Zhen
Summary: Baicalein and wogonin, as important flavonoid compounds isolated from Scutellaria baicalensis, have diverse applications in drug discovery. Derivatives of baicalein and wogonin with anticancer, anti-inflammatory, antiviral, antimicrobial, and hypoglycemic activities have been synthesized and extensively studied. This article provides a comprehensive review of the biological activities and structure-activity relationship (SAR) of baicalein and wogonin derivatives, as well as the bioactive molecules reported in patents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Asmaa M. Fahim, Eman H. I. Ismael, Ghada H. Elsayed, Ahmad M. Farag
Summary: In this study, a series of heterocyclic compounds were synthesized using microwave irradiation and their antimicrobial and antitumor activities were evaluated through experimental and theoretical studies. The compounds showed promising inhibitory effects against cancer cells, highlighting their potential as therapeutic agents.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Materials Science, Multidisciplinary
Jiyu Li, Pengfei Zhang, Mei Yang, Zixu Xie, Guofeng Li, Xing Wang
Summary: This study investigates the antimicrobial properties of polyethylene terephthalate (PET) modified with menthoxytriazine. The results show that the modified PET, named PEMT, exhibits enhanced antibacterial and antifungal performance, while also being noncytotoxic to human cells.
ACS APPLIED POLYMER MATERIALS
(2022)
Article
Biophysics
Emanuelle D. Freitas, Rogerio A. Rataglioli, Josephine Oshodi, Marisa M. Beppu
Summary: The coronavirus pandemic has highlighted the importance of bioactive materials in mitigating viral infections. Bioinspired antimicrobial peptides (AMPs) have emerged as suitable building blocks for antimicrobial coatings due to their versatile design and environmentally friendly features. This review discusses the advances and opportunities in using AMPs to create virucidal coatings, including the fundamental characteristics of peptide structure, advances in coating medical devices, and the role of different materials in designing antiviral coatings.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2022)
Article
Chemistry, Physical
Yuan-Yuan Feng, Chang-E Dong, Rui Li, Xiao-Qing Zhang, Wei Wang, Xing-Rui Zhang, Wei -Wei Liu, Da-Hua Shi
Summary: A series of new hybrids of 1,2,4-triazine-quinoline were designed, synthesized, and evaluated as antimalarial agents. The structures of these hybrids were confirmed, and compound 5c exhibited the best inhibitory activity.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Review
Chemistry, Medicinal
Bahare Salehi, Joara Nalyda Pereira Carneiro, Janaina Esmeraldo Rocha, Henrique Douglas Melo Coutinho, Maria Flaviana Bezerra Morais Braga, Javad Sharifi-Rad, Prabhakar Semwal, Sakshi Painuli, Laila Moujir Moujir, Victoria de Zarate Machado, Shriyaa Janakiram, Nanjangud Venkatesh Anil Kumar, Miquel Martorell, Natalia Cruz-Martins, Marc El Beyrouthy, Carmen Sadaka
Summary: Astragalus L. is a widely distributed genus used in folk medicine, dietary supplements, cosmetics, and animal forage. Its major phytoconstituents, including saponins, flavonoids, and polysaccharides, exhibit promising biological activities such as antiaging, antitumor, and immune-enhancing properties. This review provides a comprehensive overview of Astragalus species and their active components for future clinical development.
PHYTOTHERAPY RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Tarek E. Khalil, Kholood A. Dahlous, Saied M. Soliman, Nessma A. Khalil, Ayman El-Faham, Ali El-Dissouky
Summary: Three heteroleptic Cu(II) complexes were synthesized using two ligands, and their structures were characterized. Complex 1 showed the best anticancer activity against lung carcinoma cells and also exhibited high antioxidant activity. Complex 2 demonstrated broad-spectrum antimicrobial action against various microbes.
Review
Chemistry, Applied
Shijie (Gabriel) Kou, Linda Peters, Michael Mucalo
Summary: This article discusses the various applications of chitosan, including its antimicrobial properties, wound healing promotion, and effects on cancer and the immune system. By introducing the molecular chain configuration model, the mechanisms of interactions between chitosan and bacteria, cancer, and wound healing are explained. The article concludes that chitosan is an important polymer with promising potential in medicine due to its multiple beneficial bioactivities and mechanisms of action.
CARBOHYDRATE POLYMERS
(2022)
Article
Microbiology
Pengfei She, Yifan Yang, Linhui Li, Yimin Li, Shasha Liu, Zehao Li, Linying Zhou, Yong Wu
Summary: This study found that the antimalarial agent TAF showed antimicrobial efficacy against methicillin-resistant Staphylococcus aureus (MRSA) and its highly resistant phenotypes of biofilm and persister cells. TAF exerted its antimicrobial activity mainly through selective bacterial cell membrane disruption. It also exhibited effective antimicrobial effect in an animal model of subcutaneous abscess. These findings suggest that TAF has the potential to be developed as a new antimicrobial agent to treat refractory MRSA infections.
Article
Chemistry, Multidisciplinary
Runjhun Tandon, Iqubal Singh, Vijay Luxami, Nitin Tandon, Kamaldeep Paul
Article
Chemistry, Analytical
Gulshan Kumar, Kamaldeep Paul, Vijay Luxami
SENSORS AND ACTUATORS B-CHEMICAL
(2018)
Article
Chemistry, Multidisciplinary
Gulshan Kumar, Richa Goel, Kamaldeep Paul, Vijay Luxami
Review
Pharmacology & Pharmacy
Runjhun Tandon, Vijay Luxami, Harmanjit Singh Dosanjh, Nitin Tandon, Kamaldeep Paul
CURRENT DRUG DELIVERY
(2018)
Article
Chemistry, Physical
Simranjit Singh, Narinder Arora, Kamaldeep Paul, Rajiv Kumar, Rajesh Kumar
Article
Chemistry, Medicinal
Iqubal Singh, Richa Rani, Vijay Luxami, Kamaldeep Paul
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Chemistry, Physical
Ruhi Mehta, Pawandeep Kaur, Diptiman Choudhury, Kamaldeep Paul, Vijay Luxami
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY
(2019)
Article
Chemistry, Physical
Gulshan Kumar, Richa Rani, Kamaldeep Paul, Vijay Luxami
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY
(2019)
Article
Chemistry, Organic
Mohamad Yusuf, Shehneela Nisa, Kamaldeep Paul
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2019)
Article
Chemistry, Medicinal
Iqubal Singh, Vijay Luxami, Kamaldeep Paul
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Biochemistry & Molecular Biology
Iqubal Singh, Vijay Luxami, Kamaldeep Paul
BIOORGANIC CHEMISTRY
(2020)
Article
Chemistry, Inorganic & Nuclear
Dharmender Sharma, Jerry P. Jasinski, Victoria A. Smolinski, Manpreet Kaur, Kamaldeep Paul, Rekha Sharma
INORGANICA CHIMICA ACTA
(2020)
Article
Spectroscopy
Iqubal Singh, Vijay Luxami, Kamaldeep Paul
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2020)
Article
Chemistry, Organic
Iqubal Singh, Vijay Luxami, Kamaldeep Paul
ORGANIC & BIOMOLECULAR CHEMISTRY
(2019)
Article
Chemistry, Multidisciplinary
Pranshu Puri, Gulshan Kumar, Kamaldeep Paul, Vijay Luxami
NEW JOURNAL OF CHEMISTRY
(2018)
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)