Article
Chemistry, Organic
Hui Wang, Zhiyuan Liu, Qifan Yang, Yong Wang, Yongdan Chen, Yongqi Bao, Hongjun Zhu
Summary: An efficient method for the synthesis of arylketones via quinazoline-assisted ortho-aroylation has been developed using Pd(OAc)2 as the catalyst and tert-butyl hydroperoxide (TBHP) as the oxidant. The reaction provides good yields of up to 90% and exhibits excellent functional group tolerance and substrate scope. Radical trapping and control experiments suggest the involvement of a benzoyl radical pathway in the aroylation reaction.
TETRAHEDRON LETTERS
(2023)
Article
Chemistry, Physical
Igor Beckers, Besir Krasniqi, Prashant Kumar, Daniel Escudero, Dirk De Vos
Summary: Two indoles linked by a C-C bond have emerged as promising scaffolds in medicinal chemistry. In this study, selective C-H/C-H cross-coupling of N-substituted indoles without directing groups was achieved under mild conditions, driven by molecular oxygen. The ligand-controlled selectivity can be exploited to achieve selective cross-coupling between two indoles with different substitution patterns.
Article
Chemistry, Organic
Yuxin Ding, Huihui Yan, Rener Chen, Xuqiong Xiao, Zhiming Wang, Lei Wang, Yongmin Ma
Summary: The paper discusses a novel one-pot cascade reaction catalyzed/oxidized by the [Pd]/[Ag] system, involving two C-N bond and one C-C bond formations during the double annulation process to yield the desired products. The method is applicable to a wide range of readily available substrates and provides high yields.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Organic
Yong Wang, Hui Wang, Qifan Yang, Shihua Xie, Hongjun Zhu
Summary: An efficient method for the ortho-halogenation of 2-arylquinazolines has been developed using N-halosuccinimides as halogen sources with Pd(II)-catalyzed C-H bond activation. The protocol is highly regioselective and yields up to 98% can be achieved. The mechanism of the quinazoline ortho-halogenation was investigated through comprehensive experimentation.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Applied
Shili Guo, Haiming Zhou, Xin Huang, Siyan Peng, Jiayi Li, Bo Ding, Yiwen Tao, Hongbo Huang
Summary: Two new glucosidated indole-containing quinazoline alkaloids, designated fumigatosides G (1) and H (2), were isolated from the mangrove-derived fungus Aspergillus fumigatus SAl12, along with the known analogues fumigatoside B (3) and fumiquinazoline J (4). The planar structures of the new compounds were determined by HR-MS and NMR spectroscopy, and the absolute configurations were determined using electronic circular dichroic (ECD) spectra and comparison with a known compound. All the indole-quinazoline compounds were tested for antibacterial and cytotoxic activities.
NATURAL PRODUCT RESEARCH
(2023)
Article
Chemistry, Physical
Qiaohong Geng, Yanyan Dong, Peng Jin, Xigui Mu, Ning Zhao, Haijie Cui, Qihu Yang, Boya Xiao, Furong Zhao, Yunxiao Lv, Gaoxing Su, Guoying Wu, Peifu Jiao
Summary: Novel indole derivatives were synthesized and evaluated as PD-L1 inhibitors for cancer immunotherapy. Compound 16, identified through structure-based design and biological evaluation, showed potent inhibition of PD-1/PD-L1 interaction and enhanced cytotoxicity of CD8+ T cells against cancer cells through non-covalent aggregation of PD-L1.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Microbiology
Sha-Sha Liu, Li Yang, Fan-Dong Kong, Jia-Hui Zhao, Li Yao, Zhi-Guang Yuchi, Qing-Yun Ma, Qing-Yi Xie, Li-Man Zhou, Meng-Fei Guo, Hao-Fu Dai, You-Xing Zhao, Du-Qiang Luo
Summary: By feeding tryptophan to the marine-derived fungus Aspergillus sp. HNMF114 from the bivalve mollusk Sanguinolaria chinensis, 3 new quinazoline-containing indole alkaloids were obtained, with compound 3 showing a unique structure and promising bioactivities.
FRONTIERS IN MICROBIOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Prantika Bhattacharjee, Anindita Dewan, Purna K. Boruah, Manash R. Das, Utpal Bora
Summary: This study presents a green and rapid assessment of lignocellulosic nanomaterials derived from waste fibrous feedstock of pomegranate peels. The use of lignocellulose as a support material for Pd nanoparticles enables the catalytic C2-H arylation of indoles with arylboronic acids with high regioselectivity and reusability. The catalyst also shows good functionality tolerance for free N-H indole moieties and can be used for selective double-functionalization of indole frameworks in a one-pot system.
SUSTAINABLE CHEMISTRY AND PHARMACY
(2023)
Article
Immunology
Shu Song, Haicheng Tang, Wenqiang Quan, Anquan Shang, Chunhua Ling
Summary: This study reveals the critical roles of the E2/ERR/SIRT1/FOXO3a/PD-L1 axis in the immune escape of NSCLC cells and suggests that it could be a promising therapeutic target for NSCLC.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Jingjing Yao, Min Huang, Qinghong Shen, Ming Ding, Shaofang Yu, Yajuan Guo, Yuefang Lin, Yaqiu Zheng, Wenbo Chen, Wenxin Yan, Zhongqiu Liu, Dawei Wang, Ming Hu, Linlin Lu
Summary: Pancreatic cancer has a low overall survival rate and is often resistant to the first-line drug, Gemcitabine. This study found that c-Myc and PD-L1 were highly expressed in pancreatic tumors and dFdC-resistant cells. Moreover, the combination of dFdC and c-Myc inhibitors enhanced drug sensitivity, while overexpression of c-Myc reduced sensitivity. Additionally, ARTS was shown to reverse dFdC resistance in vitro and suppress pancreatic cancer in vivo.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Dong Hoon Shin, Jeong Yeon Jo, Minyoung Choi, Kyung-Hee Kim, Young-Ki Bae, Sang Soo Kim
Summary: The interaction between SIRT1 and p300 in KRAS-mutant lung cancer cells plays a critical role in tumor progression, suggesting the potential use of SIRT1 inhibitors and p300 activators in combination therapy for KRAS-mutant lung cancer patients.
EXPERIMENTAL AND MOLECULAR MEDICINE
(2023)
Review
Cell Biology
Wei Fan, Xiaoling Li
Summary: SIRT1 is a crucial NAD(+)-dependent protein deacetylase in mammals, involved in the metabolic and epigenetic regulation of stem cells through deacetylation of transcriptional factors and co-factors. It forms a positive feedback loop with c-Myc, which is important in tumorigenesis. Recent research has uncovered the significance of the SIRT1-c-Myc axis in the regulation of maintenance and differentiation of various stem cells. This review highlights the recent advances in understanding the role of the SIRT1-c-Myc axis in stem cells.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Kevin J. Gonzalez, Alexander W. Rand, Brian M. Stoltz
Summary: The Petasis-type reaction is a useful method for C-C bond formation in organic synthesis, but it has been limited by the need for a directing heteroatom. In this study, a non-directed Petasis-type reaction was developed, which allows for the coupling of trifluoroborate salts with alpha-hydroxyindoles. By disrupting aromaticity and using trifluoroborate nucleophiles, a new C-C bond can be generated without a directing group. This reaction is simple and efficient, and it has been applied as a bioconjugation strategy and for the synthesis of non-natural bisindole alkaloid analogs.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Organic
An-Xiang Huang, Hu-Lin Zhu, Fan-Lin Zeng, Xiao-Lan Chen, Xian-Qiang Huang, Ling-Bo Qu, Bing Yu
Summary: 1-Acryloyl-2-cyanoindoles were discovered to be novel and efficient scaffolds in visible-light-induced persulfate-promoted cascade cyclization reactions. With this transition-metal-free photocatalytic procedure, various sulfonated/thiocyanated pyrrolo[1,2-a]indolediones were synthesized from 1-acryloyl-2-cyanoindoles with sulfonyl hydrazides/NH4SCN at room temperature under mild reaction conditions.
Article
Chemistry, Organic
Luyao Liu, Jingyang Lin, Mingxuan Pang, Huile Jin, Xiaochun Yu, Shun Wang
Summary: A novel photo-thermo-mechanochemical approach has been developed to assemble quinolines catalyzed by iron(II) phthalocyanine, featuring a cost-efficient catalytic system with operational simplicity and solvent-free conditions. Mechanistic experiments suggest that the in-situ-formed secondary amine may play a key role in the further cyclization/aromatization process.
Article
Multidisciplinary Sciences
Shovan Dogra, Madhumangal Pal
Summary: This paper introduces the concept of picture fuzzy subring of a crisp ring and studies some basic results. The properties of picture fuzzy subring under classical ring homomorphism are also investigated.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES INDIA SECTION A-PHYSICAL SCIENCES
(2021)
Article
Chemistry, Organic
G. Dhananjaya, Akula Raghunadh, P. Mahesh Kumar, S. Pulla Reddy, V. Narayana Murthy, Venkateswara Rao Anna, Manojit Pal
Summary: Polyhydroquinolines were synthesized via Hantzsch's multicomponent reaction using urea as an effective ammonia surrogate under green conditions. The reaction afforded a range of products depending on the nature of reaction conditions employed.
LETTERS IN ORGANIC CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Ban-Feng Ruan, Qing-Lei Guo, Qing-Shan Li, Lu-Zhi Li, Girdhar Singh Deora, Ben-Guo Zhou
Summary: The oxadiazole core is widely used in medicinal chemistry and compounds containing oxadiazole rings have diverse biological activities. The 1,3,4-oxadiazole moiety has been extensively explored in medicinal chemistry research.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Analytical
Sagnik Das, Subhajit Mojumder, Debdulal Saha, Mrinal Pal
Summary: In this review, the significant effects of various parameters on the sensing behavior of semiconductor metal oxide (SMO) based chemiresistive gas sensors have been discussed in detail. The study systematically reviewed the impact of different material and operating condition aspects on the gas sensing performance of SMO sensors. The importance of long-term stability and high-throughput synthesis techniques in practical applications was emphasized, and the future prospects of SMO-based sensors in personalized healthcare were briefly outlined.
SENSORS AND ACTUATORS B-CHEMICAL
(2022)
Article
Chemistry, Organic
Sailaja Garrepalli, Ramesh Gudipati, Kunta Ravindhranath, Manojit Pal
Summary: This article presents new synthetic methods for the enantiomer (4S, 12aR) and ethoxy acetamide, as well as an environmentally friendly alternative for the synthesis of impurity B. The synthesized impurities were characterized and analyzed, confirming the feasibility and suitability of the developed methods.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Chemistry, Physical
Tanushri Das, Subhajit Mojumder, Sonam Chakraborty, Debdulal Saha, Mrinal Pal
Summary: Pure and Sn-doped Bismuth Ferrite (BFO) nanoparticles were synthesized and their gas sensing properties towards formaldehyde were investigated. The Sn-doped BFO nanoparticles showed enhanced formaldehyde sensing performance, with high selectivity and fast response/recovery time. The detection limit of the prepared sensors was low, making them a potential candidate for monitoring formaldehyde in indoor and outdoor air quality.
APPLIED SURFACE SCIENCE
(2022)
Article
Materials Science, Ceramics
Sonam Chakraborty, Nirman Chakraborty, Swastik Mondal, Mrinal Pal
Summary: This study reports the efficient photocatalytic degradation of methyl blue dye using Sn-doped bismuth ferrite nanoparticles under visible light. The 1.5% Sn-doped BFO nanoparticles exhibited the highest photocatalytic activity, degrading 70% of the dye within 10 minutes of visible light irradiation. These nanoparticles also showed potential for degrading another important contaminant, RhB.
CERAMICS INTERNATIONAL
(2022)
Article
Chemistry, Medicinal
Julia Beveridge, Eric Tran, Girdhar Singh Deora, Fei Huang, Yuzhi Wang, Kieran Stockton, Ignacio Cotillo, Maria Santos Martinez Martinez, Silvia Gonzalez, Pablo Castaneda, Julian Sherman, Ana Rodriguez, Albane Kessler, Jonathan B. Baell
Summary: This article describes the hit optimization of a novel diarylthioether chemical class that is active against Trypanosoma cruzi, the parasite responsible for Chagas disease. The hit compound was discovered through a whole-cell phenotypic screen and its mechanism of action remains unknown. The study reveals clear structure-activity relationships and the identification of analogues with high in vitro potency. Additionally, the diarylthioether compounds demonstrate promising activity in in vivo efficacy studies in mice infected with transgenic T. cruzi. These findings suggest that further development of these compounds is warranted for Chagas disease drug discovery to improve oral exposure without increasing toxicity.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Analytical
Subhajit Mojumder, Tanushri Das, Sagnik Das, Nirman Chakraborty, Debdulal Saha, Mrinal Pal
Summary: This study presents a highly sensitive and selective Al and Y co-doped ZnO nanopowder sensor for detecting trace ethanol in exhaled breath. The sensor exhibits rapid response and recovery time, good repeatability, and long-term stability, as well as excellent selectivity towards ethanol. It has the potential to be used for detecting liver problems and for breathalyzer testing in cases of drunken driving.
SENSORS AND ACTUATORS B-CHEMICAL
(2022)
Article
Chemistry, Multidisciplinary
Snehasis Mishra, Kaustav Das, Sujan Chatterjee, Panchanan Sahoo, Sudip Kundu, Mrinal Pal, Asim Bhaumik, Chandan Kumar Ghosh
Summary: Carbon dots (CQDs) with tunable fluorescence emission and excitation, high water solubility, good photostability, and biocompatibility are considered promising for tumor theranostics. This study focused on the synthesis and characterization of highly fluorescent CQDs from orange juice. CQD/Ag heterostructures were also synthesized and their photostability and characterization were investigated. Cellular toxicity measurements were conducted to select the superior CQD/Ag heterostructure in the human colorectal carcinoma (HCT 116) cell line, along with the observation of cell death signaling through the ROS-dependent mitochondrial-mediated pathway.
Article
Chemistry, Multidisciplinary
Monalisa Adhikari, Sagnik Das, Dipankar Chattopadhyay, Debdulal Saha, Mrinal Pal
Summary: Recently, there has been significant interest in the precise detection of VOCs, especially acetone, ammonia, and alcohol, due to their importance in industrial safety, environmental monitoring, and human health. This article reports on a chemiresistive sensor based on polypyrrole nanotubes (PPNT) for the selective detection of trace acetone vapor at room temperature. The PPNT sensor demonstrated a high response to trace acetone vapor with a low detection limit and quick response and recovery times.
Article
Chemistry, Multidisciplinary
Banoth Reddy, Amit Kumar Taneja, Mandava Bhuvan Tej, Komati Navya Sri, Mandava Bhagya Tej, Suryadevara Vijayavardhini, Dandamudi Srilaxmi, Somasekhar Tiruveedhula, Srinivasa Rao Penumutchu, Mandava V. Basaveswara Rao
Summary: Novel tetrazole fused imidazopyridine derivatives were synthesized and tested for their cytotoxic activity against cancer cell lines. Compounds 12 h and 12j showed strong anticancer activity against A549 cell line.
Article
Chemistry, Multidisciplinary
Narender Addu, Hinuja Miriyala, Ravikumar Kapavarapu, Sunder Kumar Kolli, Manojit Pal
Summary: The synthesis of spiroindoline-3,2'-quinazoline derivatives using Wang-OSO3H as a catalyst and their evaluation against MtbCM (Mycobacterium tuberculosis Chorismate Mutase) in silico and in vitro are reported. The docking studies revealed the binding of these compounds on the external surface pockets of the MtbCM active site cavity.
Article
Chemistry, Multidisciplinary
Gangireddy Sujeevan Reddy, Sharda Shukla, Harshavardhan Bhuktar, Kazi Amirul Hossain, Rebecca Kristina Edwin, Varadaraj Bhat Giliyaru, Parimal Misra, Manojit Pal
Summary: In this study, structurally similar benzofuran derivatives were designed and evaluated for their inhibitory activity against chorismate mutase. The molecules showed strong interactions with the target enzyme and were synthesized in high yields. Three compounds exhibited promising inhibition in vitro and could be of interest in the development of new anti-tubercular agents.
Article
Chemistry, Multidisciplinary
Sagnik Das, Uttam K. Ghorai, Rajib Dey, Chandan K. Ghosh, Mrinal Pal
Summary: This study reports the achievement of highly reproducible, stable, and intense white phosphorescence from phase-pure zinc oxide nanopowder synthesized by a simple, low temperature process. The white light emission has appreciable quantum yield and cool/near cool correlated color temperature, making it suitable for W-LED applications. The presence of zinc interstitial and oxygen interstitial defects responsible for the white phosphorescence was confirmed, and a defect chemistry-based thermodynamic interpretation was proposed to explain the white emission adequately.
NEW JOURNAL OF CHEMISTRY
(2022)
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)
