Article
Biochemistry & Molecular Biology
Shun Tu, Ting-Jian Zhang, Yi Zhang, Xu Zhang, Zhen-Hao Zhang, Fan-Hao Meng
Summary: This study synthesized two series of amide-based XO inhibitors, with compound 3i showing the most promising in vitro inhibitory potency and hypouricemic effect. Molecular simulations provided insights into the interaction modes of representative compounds, supporting compound 3i as a lead for further exploration of amide-based XO inhibitors.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Aonan Ren, Wanxing Wei, Zhengcheng Liang, Min Zhou, Taoyuan Liang, Ning Zang
Summary: Based on the inhibitory effect on tubulin polymerization, a series of N-((1-methyl-1H-indol-3-yl)methyl)-2-(1H-pyrazol-1-yl or triazolyl)-N-(3,4,5-trimethoxyphenyl)acetamides were designed and synthesized. These compounds showed effective antiproliferative activities against HeLa, MCF-7, and HT-29 cancer cell lines. Compound 7d demonstrated the most potent activities and induced cell apoptosis, arrested cells in the G2/M phase, and inhibited tubulin polymerization similar to colchicine. Therefore, compound 7d is a potential agent for the development of tubulin polymerization inhibitors.
RSC MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Organic
Chunhua Ma, Yue Wang, Guang Chen, Jingyi Li, Yuqin Jiang, Xinying Zhang, Xuesen Fan
Summary: This paper presents the synthesis of 3-(indol-2-yl)succinimide/maleimide and indoyl/pyrrolyl fused benzodiazepine skeletons through the reaction of 2-(1H-indol-1-yl)anilines with maleimides. Mechanistic studies reveal that the formation of these compounds involves Ru(ii)-catalyzed and free amino group-assisted regioselective bond cleavage and coordination reactions. The synthesized compounds show potential as lead compounds for the development of anticancer drugs.
ORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Biochemistry & Molecular Biology
Alexander Aksenov, Nicolai A. Aksenov, Elena Aleksandrova, Dmitrii A. Aksenov, Igor Yu Grishin, Elena A. Sorokina, Allison Wenger, Michael Rubin
Summary: The [4+1]-spirocyclization of nitroalkenes to indoles provides a convenient approach to 2-(1H-indol-2-yl)acetonitriles, but can lead to unwanted byproducts. This study offers a solution to effectively transform these byproducts into the desired acetonitrile molecules.
Article
Biochemistry & Molecular Biology
Igor Yu Grishin, Nikolai A. Arutiunov, Dmitrii A. Aksenov, Nicolai A. Aksenov, Alexander Aksenov, Amina Z. Gasanova, Elena A. Sorokina, Carolyn Lower, Michael Rubin
Summary: In this study, polyphosphoric acid was used as a catalyst to efficiently synthesize 3-(1H-indol-3-yl)benzofuran-2(3H)-ones via condensation reaction between 3-(2-nitrovinyl)-1H-indoles and phenols.
Article
Chemistry, Multidisciplinary
Hisashi Masui, Sena Kanda, Shinichiro Fuse
Summary: The authors examined previously reported preparations of (1H-indol-3-yl)methyl halides, clarified inconsistencies within the literature, and developed a highly versatile nucleophilic substitution method using microflow technologies, enabling the synthesis of various indole derivatives.
COMMUNICATIONS CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Nan-Sheng Li, Joseph A. Piccirilli, Geoffrey L. Greene
Summary: We have reexamined the reported method for the synthesis of MIBE and identified a different product based on NMR and MS data.
Article
Chemistry, Medicinal
H. C. Yuan, L. X. Xu, N. H. Wang, H. B. Leng, S. W. Que
Summary: This study discovered a compound named SNA that has inhibitory effects on neuroglioma by increasing apoptosis to suppress cell proliferation and migration. This suggests that SNA has the potential to be a drug for treating neuroglioma.
PHARMACEUTICAL CHEMISTRY JOURNAL
(2022)
Article
Medicine, Research & Experimental
Aichun Li, Qin Yang, Guohua Lou, Yanning Liu, Hongguang Xia, Zhi Chen
Summary: In this study, F-nec was identified as a novel potent RIP1 inhibitor that efficiently blocked TNF-alpha-induced necroptosis in human and mice cells. Pre-treatment with F-nec prevented hepatic necrosis and attenuated LPS/GalN-induced acute liver failure by suppressing JNK-triggered inflammation, highlighting its potential for use in the treatment of inflammatory liver diseases driven by RIP1.
Article
Biochemistry & Molecular Biology
Ningning Cheng, Nan Jiang, Yuanhui Fu, Zhuxin Xu, Xianglei Peng, Jiemei Yu, Shan Cen, Yucheng Wang, Guoning Zhang, Yanpeng Zheng, Jinsheng He
Summary: Human respiratory syncytial virus (RSV) is a major cause of lower respiratory tract infection worldwide, and there are currently no licensed vaccines or effective antiviral drugs against it. A study found that a novel inhibitor showed activity against RSV replication in vitro, but failed to inhibit RSV infection in mice, possibly due to rapid metabolism in vivo. Further modification and optimization of this inhibitor's structure is necessary to develop candidates with effective anti-RSV activity in vivo.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
John Saathoff, Jakob Green, Yuqi Jiang, Yiming Xu, Glen E. Kellogg, Shijun Zhang
Summary: This study focused on developing novel neuroprotectants for Alzheimer's disease by synthesizing analogs based on a lead compound that targets mitochondrial complex I. Results from cellular AD models and docking studies supported the importance of specific structural features for neuroprotective activities. The findings provide valuable information for optimization and development of analogs with a novel mechanism of action for AD.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Food Science & Technology
Kang Li, Dawei Yuan, Wei Chen, Rulan Ma, Yinsheng Xian
Summary: A new compound called (S)-(-)-N-[2-(3-Hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)-ethyl]-acetamide (EA), isolated from Selaginella pulvinata, has been found to possess anti-proliferative effects against SK-mel-110 cells. In this study, EA was investigated for its potential antitumor effects against colon cancer. The results showed that EA could induce apoptosis of colon cancer cells and inhibit colon tumor growth in mouse models. Additionally, EA treatment also affected the tumor microenvironment by reducing suppressor cell accumulation and increasing tumor infiltrating lymphocytes.
FOOD SCIENCE AND TECHNOLOGY
(2022)
Article
Chemistry, Medicinal
Monika Iskauskiene, Alena Kadlecova, Jiri Voller, Lucie Janovska, Vida Malinauskiene, Asta Zukauskaite, Algirdas Sackus
Summary: A small library of 2-[(1H-indol-3-yl)methyl]-5-(alkylthio)-1,3,4-oxadiazoles was prepared and screened for protective effects in vitro and in vivo. The compounds showed protective effects against glutathione depletion induced by an inhibitor, as well as increased survival of Caenorhabditis elegans under oxidative stress.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Multidisciplinary
Velmurugan Tamilselvi, Cinnathambi Subramani Maheswari, Appaswami Lalitha
Summary: A new, efficient one-pot three-component synthesis of oxindole derivatives has been developed, offering excellent yields, shorter reaction time, readily available starting materials, and mild reaction conditions. This method avoids the use of expensive catalysts and toxic solvents, making it a simple and effective synthetic approach.
JOURNAL OF THE IRANIAN CHEMICAL SOCIETY
(2022)
Article
Pharmacology & Pharmacy
Jianyuan Zhao, Guoning Zhang, Yongxin Zhang, Dongrong Yi, Quanjie Li, Ling Ma, SaiSai Guo, Xiaoyu Li, Fei Guo, Rongtuan Lin, Gia Luu, Zhenlong Liu, Yucheng Wang, Shan Cen
Summary: SARS-CoV-2 RdRp shows potential as a reliable target for antiviral drug development. Effective therapies are urgently needed to combat the COVID-19 pandemic.
ANTIVIRAL RESEARCH
(2021)