Article
Biochemistry & Molecular Biology
Manpreet Kaur, Vikrant Mehta, Aabid Abdullah Wani, Sahil Arora, Prasad Bharatam, Ashoke Sharon, Sandeep Singh, Raj Kumar
Summary: A new synthetic route for 1,4-dihydropyrazolo[4,3-b]indoles was reported, and the resulting compounds showed cytotoxicity against various cancer cell lines, potentially acting as selective inhibitors of Topo I or Topo II.
BIOORGANIC CHEMISTRY
(2021)
Article
Nanoscience & Nanotechnology
Haney Lee, Subin Chae, Hyemi Jo, Semin Kim, Minjin Kim, Jisun Lee, Sanghyuck Lee, Hyeonseok Yoon, Chul Soon Park
Summary: This study proposes an efficient strategy for selectively detecting isothiazolinones using nanohybrid transducers. Chemical receptor candidates were designed and synthesized, and anchored to graphene for electrochemical transduction. By adjusting the potential of the transducers, the detection of isothiazolinones can be achieved.
ACS APPLIED NANO MATERIALS
(2022)
Article
Biochemistry & Molecular Biology
Rafaela G. Cabral, Goncalo Viegas, Rita Pacheco, Ana Catarina Sousa, Maria Paula Robalo
Summary: This study describes the sustainable synthesis, characterization, and evaluation of the electrochemical and biological properties of different substituted derivatives of 1,4- and 1,2-naphthoquinones (NQ). The synthesis of the derivatives was optimized using a microwave-assisted protocol, providing a more sustainable approach. The compounds were found to have potential anti-cancer activity against HepG2 cell lines and inhibitory action against AChE enzymes. Docking studies showed different binding interactions for the derivatives.
Article
Chemistry, Medicinal
Xin Chen, Jiayun Wang, Peng Zhao, Baiyun Dang, Ting Liang, Raphael R. Steimbach, Aubry K. Miller, Jia Liu, Xin Wang, Tongtong Zhang, Xiaofa Luan, Jiadong Hu, Jinming Gao
Summary: In this study, a series of novel selective HDAC6 inhibitors were designed and synthesized, showing good anti-proliferative activity against multiple tumor cell lines and high selectivity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Muhammed Tilahun Muhammed, E. R. Mustafa, Senem Akkoc
Summary: Five compounds were synthesized and tested for their antiproliferative activities against two cancer cell lines. Compound 2b, which contains an imidazole core, showed the highest cytotoxic activity in both cell lines after 24 and 48 hours of incubation. The binding potential of 2b with topoisomerase I was assessed through molecular docking and the stability of the complexes was investigated through molecular dynamics simulations. Computational pharmacokinetics analysis revealed that 2b could bind to topoisomerase I, but to a lesser extent than the reference drug. In silico pharmacokinetics also showed that the synthesized compounds had drug-like properties.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Physical
Jayashree Ethiraj, R. Ajin, R. K. Sankaranarayanan, Ranjith Sekar, Dhinakaran Veeman, Moola Joghee Nanjan, Jithin John Varghese
Summary: Single crystals of two 1,4-dihydropyridine derivative molecules were prepared, and their crystal structures were analyzed using Hirshfeld surface analysis. The relative contributions of intermolecular contacts to the surface area were determined, and the molecular structures were optimized and confirmed by Density Functional Theory simulations. The molecular electrostatic potential and frontier molecular orbital analysis provided insights into the reactivity and stability of the molecules.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Vo Ngoc Binh, Sabrina Adorisio, Domenico Delfino, Quoc Anh Ngo
Summary: The research focuses on multitargeting drugs and the discovery of agents that can act on multiple biological targets. In this study, a novel synthetic route to fused-heterocycles, 1,4-dihydropyrazolo[4,3-b]indoles, was reported. Two lead compounds, 3b and 4b, showed significant inhibition of cell growth, induced apoptosis in leukemia cells, and decreased levels of tumor necrosis factor-alpha and transforming growth factor-beta. These compounds have potential as novel anticancer agents.
NATURAL PRODUCT COMMUNICATIONS
(2022)
Article
Chemistry, Organic
Pingshun Zhang, Linjie Yang, Wanzhi Chen, Miaochang Liu, Huayue Wu
Summary: An efficient method for the synthesis of [1,4]thiazino[4,3-alpha]indole derivatives was developed using sodium chlorodifluoroacetate and elemental sulfur as the difluoromethylthiolating reagent system. The sequential transformation process selectively formed four bonds including one C-N, two C-S, and one C-C bonds in good yields.
Article
Chemistry, Medicinal
Man-Yu Lin, Tang-Yang Ji, Miao Zheng, Yan-Yan Chen, Shi-Yi Xu, Wen-Wei You, Pei-Liang Zhao
Summary: A novel series of 6-arylamino-[1,2,4]triazolo[4,3-a]pyridine derivatives were synthesized and evaluated for their antiproliferative activities. Inserting an amino linkage between the 6-aryl group and [1,2,4]triazolo[4,3-a]pyridine core resulted in a broader antitumor spectrum. Compound 8l exhibited potent and broad-spectrum antiproliferative activity, inducing cell cycle arrest and apoptosis. These findings suggest significant potential for the discovery of new highly efficient anticancer agents.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Engineering, Chemical
Yansu Lan, Die Zhou, Longhuan Lai, Huanhuan Qi, Lei Xia, Stef Depuydt, Bart Van der Bruggen, Yan Zhao
Summary: Membrane technology has great potential in bromide recovery, and a class of novel anion exchange membranes (AEMs) fabricated through chemical substitution reaction showed better performance in bromide recovery and higher selectivity.
SEPARATION AND PURIFICATION TECHNOLOGY
(2023)
Article
Medicine, Research & Experimental
Juliana Alves do Vale, Michelle Peixoto Rodrigues, Angela Maria Almeida Lima, Samira Soares Santiago, Graziela Domingues de Almeida Lima, Alisson Andrade Almeida, Leandro Licursi de Oliveira, Gustavo Costa Bressan, Robson Ricardo Teixeira, Mariana Machado-Neves
Summary: Melanoma, the most aggressive skin cancer, has been increasing in incidence over the past decades. Conventional treatments have severe side effects and melanoma can be resistant to commonly used anticancer drugs, necessitating the search for new potential anti-melanoma drugs. In this study, we synthesized seventeen compounds derived from cinnamic acid and evaluated their bioactivity against melanoma cells. Phenyl 2,3-dibromo-3-phenylpropanoate (3q) was found to be the most effective compound against murine B16-F10 cells, showing cytotoxicity and inhibitory effects on cell migration. It also had low cytotoxicity on non-tumor cells. Additionally, compound 3q induced apoptosis at high concentrations, while affecting cell cycle and melanoma cell proliferation at lower concentrations. Furthermore, cinnamate 3q inhibited cell invasion, adhesion, colonization, and actin polymerization. These results demonstrate the antiproliferative and antimetastatic potential of cinnamic acid derivatives on melanoma.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Marianna Budovska, Radka Michalkova, Martin Kello, Janka Vaskova, Jan Mojzis
Summary: This study focuses on the synthesis of new bis-indole analogues with a phenyl linker derived from indole phytoalexins. Various synthetic methods were applied to obtain these bis-indole homodimers. Compound 49 displayed significant inhibitory effects on lung cancer cell proliferation and induced autophagy and apoptosis. It also potentiated the antiproliferative effect of cis-platin.
Article
Chemistry, Medicinal
Jinsu Bae, Koon Mook Kang, Yong-Chul Kim
Summary: This study designed and synthesized 5-methyl-1H-benzo[d]imidazole derivatives and discovered that compounds 17a and 17b exhibited strong P2X3R antagonistic activity and selectivity. The study also suggested the existence of another allosteric binding site for the novel P2X3R antagonists.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Chemistry, Applied
Slawomir Kula, Przemyslaw Ledwon, Anna M. Maron, Mariola Siwy, Justyna Grzelak, Marcin Szalkowski, Sebastian Mackowski, Ewa Schab-Balcerzak
Summary: In this study, four new 1-phenyl-1H-phenanthro[9,10-d]imidazole derivatives containing N-donor substituents at the C2 position were synthesized and characterized by high thermal stability and photoluminescence quantum yields. Their thermal, electrochemical, spectroelectrochemical, and optical properties were investigated. Additionally, their electroluminescent ability was preliminarily tested.
Article
Chemistry, Multidisciplinary
Afaf Y. Khormi, Thoraya A. Farghaly, Abrar Bayazeed, Youssef O. Al-Ghamdi, Hanan Gaber Abdulwahab, Mohamed R. Shaaban
Summary: Novel thiazole derivatives were synthesized and found to possess significant inhibitory activity against B-RAFV600E kinase, with high selectivity towards B-RAF wild type. Compounds 7b and 13a exhibited excellent inhibitory activity and showed strong anticancer activity against mutated melanoma cells.
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)