Article
Biochemistry & Molecular Biology
Hui -Hui Gao, Nai-Chang Hou, Xin Gao, Jing-Yang Yuan, Wan-Qing Kong, Chen-Xia Zhang, Zhao Qin, Hua-Min Liu, Xue-De Wang
Summary: In this study, two proanthocyanidins (PAs) with different degrees of polymerization (DP) were extracted from Chinese quince fruits and combined with bovine serum albumin (BSA). The results showed that the complexes formed by PAs and BSA had different secondary structures. Molecular docking studies indicated that hydrogen bonds and hydrophobic interactions were the forces holding the complexes together. The thermal stabilities of PAs were stronger than those of PAs-BSA, and PAs-BSA showed increased antioxidant activity with increasing temperature. Furthermore, PAs-BSA had stronger HCAs inhibition than PAs, suggesting that PAs can be used as natural antioxidants for reducing HCAs in fried foods.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Chemistry, Multidisciplinary
Eduard O. Bobylev, Renzo A. Knol, Simon Mathew, I. I. I. David A. Poole, Ioli Kotsogianni, Nathaniel I. Martin, Bas de Bruin, Alexander Kros, Joost N. H. Reek
Summary: There is a growing interest in using metal-organic cages (MOCs) in the field of biomedicine due to their unique distribution in organisms and novel cytotoxicity mechanisms. However, the stability of many MOCs under in vivo conditions hinders their study in living cells. In this study, the toxicity and photophysical properties of stable rhodamine-functionalized platinum-based Pt2L4 nanospheres and their building blocks are investigated in vitro and in vivo. The results show that the Pt2L4 nanospheres exhibit reduced cytotoxicity and altered biodistribution compared to the building blocks in zebrafish and human cancer cell lines. These findings provide a basis for the application of MOCs in cancer therapy.
Article
Biochemistry & Molecular Biology
Patricio Sanchez, Cristian O. Salas, Sebastian Gallardo-Fuentes, Alondra Villegas, Nicolas Veloso, Jessica Honores, Martyn Inman, Mauricio Isaacs, Renato Contreras, Christopher J. Moody, Jonathan Cisterna, Ivan Brito, Ricardo A. Tapia
Summary: This study describes the successful application of fragment-based drug discovery strategy to efficiently synthesize phenylamino or phenoxy-substituted benzofuran, benzoxazole, and benzothiazole quinones. Unusual results were observed in the regiochemistry of the reactions between bromoquinones and phenol/aniline during the final step of the synthesis. The findings indicate that the phenoxy quinone fragment led to compounds with increased cytotoxic activity against pancreatic cancer cells. Electrochemical properties of these quinones were also determined to understand their potential mechanism of action.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Chemistry, Multidisciplinary
Manoj Gayke, Nirbhay Hirapara, Hanuman Narode, Siddhanath D. Bhosle, Rajesh S. Bhosale, Jhillu Singh Yadav
Summary: Here, a synthetic protocol for the synthesis of carbamates using zinc chloride as a catalyst is reported. The protocol has been successfully applied to the gram-scale synthesis of FDA-approved drugs and their derivatives, with yields ranging from 49-87%. The utility of zinc chloride is demonstrated over other catalysts such as zinc dust and zinc acetate.
Article
Multidisciplinary Sciences
Robin Fertig, Felix Leowsky-Kuenstler, Torsten Irrgang, Rhett Kempe
Summary: Introducing unknown compound classes is crucial for expanding the chemical space. The authors propose a rational design concept and synthesis of unknown classes of N-heterocyclic compounds. The discovery of reactions is a central topic in chemistry, and the ability to synthesize unexplored compound classes is particularly fascinating. N-Heterocyclic compounds are highly important due to their wide applications in life and material sciences. The authors introduce a sequential three-component reaction, classes of N-heterocyclic compounds, and the regenerative cyclisation synthesis concept.
NATURE COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Lu Wang, Fuxing Shi, Chaorong Qi, Wenjie Xu, Wenfang Xiong, Bangxiong Kang, Huanfeng Jiang
Summary: The study presents a stereodivergent synthesis of beta-iodoenol carbamates through a photocatalytic three-component coupling, demonstrating the potential synthetic utility and practicality of the method. Additionally, this strategy could provide a general method for stereodivergent construction of trisubstituted alkenes, representing a fascinating challenge in the field of organic chemistry research.
Article
Chemistry, Physical
Elena Castellini, Fabrizio Bernini, Beatrice Bighi, Daniele Malferrari, Adele Mucci, Ignacio Sainz Diaz, Giulio Gorni, Maria Franca Brigatti, Marco Borsari
Summary: The capture of amines known as widespread pollutants, including aliphatic (APAs) and heterocyclic (HCAs), by Cu2+-exchanged montmorillonite (Mt-Cu) was studied using various analytical techniques. The study found that the immobilized amount of amines depended on the structure of the molecule for APAs, while it remained constant for HCAs. The coordination of Cu2+ ions to the amino groups was confirmed through spectroscopic and X-ray studies. The results supported the potential of Cu2+-modified layered silicates as an efficient air/gas purification system.
APPLIED CLAY SCIENCE
(2023)
Review
Chemistry, Applied
Lu Wang, Chaorong Qi, Wenfang Xiong, Huanfeng Jiang
Summary: Carbon dioxide (CO2) is not only the main greenhouse gas but also an ideal C1 feedstock in organic synthesis. The synthesis of organic carbamates using CO2 as a phosgene alternative has received extensive attention. This review summarizes the recent advances in the synthesis of organic carbamates from CO2 using different multicomponent reaction strategies and presents future perspectives and challenges.
CHINESE JOURNAL OF CATALYSIS
(2022)
Article
Chemistry, Organic
Miho Ibara, Takumi Abe, Daisuke Sawada
Summary: This article presents an important reaction in peptide synthesis, which distinguishes the terminal amino group and selectively transforms only the N-terminal protecting group. Furthermore, this strategy is applicable to the late stage of peptide synthesis and allows for the introduction of fluorine into peptides.
Article
Chemistry, Multidisciplinary
Katsuhiko Takeuchi, Ming-Yu Chen, Hao-Yu Yuan, Hiroki Koizumi, Kazuhiro Matsumoto, Norihisa Fukaya, Yoong-Kee Choe, Shinji Shigeyasu, Seiji Matsumoto, Satoshi Hamura, Jun-Chul Choi
Summary: The study successfully isolated and characterized a zinc carbamate complex and proposed an improved catalytic system that can efficiently synthesize various carbamates, including industrially important polyurethane raw materials, using CO2 under atmospheric pressure.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Chemistry, Multidisciplinary
Hwajin Yun, Yoonjeong Chae, Eunji Kim, Hong Ki Kim, Sukhyeun Jang, Mu-Hyun Baik, Chi Won Ahn, Yonghee Lee
Summary: This study reports a simple but effective strategy to enhance the stability of delaminated MXenes by passivating vulnerable edges with heterocyclic aromatic amines. The functionalized pyrrole MXenes exhibit long-term anti-oxidation in aqueous solutions and higher electrochemical performance as a supercapacitor.
ADVANCED FUNCTIONAL MATERIALS
(2022)
Review
Biochemistry & Molecular Biology
Hossam Nada, Ahmed Elkamhawy, Kyeong Lee
Summary: Inhibiting pathological angiogenesis is a key approach for anti-cancer drugs, requiring understanding of structure-activity relationships (SAR) and identification of broad-spectrum anti-angiogenesis targets. Heterocyclic organic compounds are the most promising anti-angiogenic drugs, with further research and optimization expected to enhance efficacy.
Article
Biochemistry & Molecular Biology
Xu Liu, Xiao-Jing Pang, Yuan Liu, Wen-Bo Liu, Yin-Ru Li, Guang-Xi Yu, Yan-Bing Zhang, Jian Song, Sai-Yang Zhang
Summary: Through the design and synthesis of a series of N-containing heterocyclic derivatives, a novel tubulin polymerization inhibitor with potential anti-tumor activity was identified, which could achieve its anti-cancer activity by inhibiting tubulin polymerization and disrupting microtubule networks.
Article
Chemistry, Multidisciplinary
Wen-si Zhao, Kai-feng Chen, Man Liu, Xing-long Jia, Yu-qi Huang, Bing-bing Hao, Hao Hu, Xiao-yan Shen, Qiang Yu, Min-jia Tan
Summary: This study systematically characterized the covalent targets and cellular pathways of Eriocalyxin B, 17-hydroxy-jolkinolide B, parthenolide, xanthatin, and andrographolide, all of which possess promising antitumor activities. The study revealed that these compounds affect the ubiquitin mediated proteolysis pathways and identified the preferentially modified targets of EB and PN. Biochemical experiments demonstrated that PN inhibits cell proliferation by targeting ubiquitin carboxyl-terminal hydrolase 10 (USP10).
ACTA PHARMACOLOGICA SINICA
(2023)
Article
Chemistry, Multidisciplinary
Yasunori Toda, Minoru Shishido, Tatsuya Aoki, Kimiya Sukegawa, Hiroyuki Suga
Summary: A base-promoted switchable synthesis of five- and six-membered cyclic carbamates using atmospheric pressure carbon dioxide as the C1 source was developed. The chemoselectivity of products was controlled by changing bases and solvents. Experimental results and DFT studies revealed the reaction mechanism.
CHEMICAL COMMUNICATIONS
(2021)
Article
Chemistry, Medicinal
Nikhil R. Madadi, Narsimha R. Penthala, Kevin Howk, Amit Ketkar, Robert L. Eoff, Michael J. Borrelli, Peter A. Crooks
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Narsimha Reddy Penthala, Hongliang Zong, Amit Ketkar, Nikhil Reddy Madadi, Venumadav Janganati, Robert L. Eoff, Monica L. Guzman, Peter A. Crooks
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Nikhil Reddy Madadi, Peter Anthony Crooks
LETTERS IN DRUG DESIGN & DISCOVERY
(2015)
Article
Biochemistry & Molecular Biology
Sravan C. Penchala, Mark R. Miller, Arindom Pal, Jin Dong, Nikhil R. Madadi, Jinghang Xie, Hyun Joo, Jerry Tsai, Patrick Batoon, Vyacheslav Samoshin, Andreas Franz, Trever Cox, Jesse Miles, William K. Chan, Miki S. Park, Mamoun M. Alhamadsheh
NATURE CHEMICAL BIOLOGY
(2015)
Article
Biochemistry & Molecular Biology
Narsimha Reddy Penthala, Leena Madhukuri, Shraddha Thakkar, Nikhil Reddy Madadi, Gauri Lamture, Robert L. Eoff, Peter A. Crooks
Article
Biochemistry & Molecular Biology
Nikhil R. Madadi, Hongliang Zong, Amit Ketkar, Chen Zheng, Narsimha R. Penthala, Venumadhav Janganati, Shobanbabu Bommagani, Robert L. Eoff, Monica L. Guzman, Peter A. Crooks
Article
Chemistry, Medicinal
Nikhil R. Madadi, Amit Ketkar, Narsimha R. Penthala, April C. L. Bostian, Robert L. Eoff, Peter A. Crooks
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2016)
Article
Oncology
Nikhil R. Madadi, Narsimha R. Penthala, Amit Ketkar, Robert L. Eoff, Vicenta Trujullo-Alonso, Monica L. Guzman, Peter A. Crooks
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2018)
Article
Crystallography
Venumadhav Janganati, Narsimha Reddy Penthala, Nikhil Reddy Madadi, Sean Parkin, Peter A. Crooks
ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE
(2014)
Article
Crystallography
Nikhil Reddy Madadi, Narsimha Reddy Penthala, Shobanbabu Bommagani, Sean Parkin, Peter A. Crooks
ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE
(2014)
Article
Chemistry, Medicinal
Nikhil Reddy Madadi, Narsimha Reddy Penthala, Venumadhav Janganati, Peter A. Crooks
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2014)
Article
Chemistry, Medicinal
Aleksandra. K. Greer, Nikhil R. Madadi, Stacie M. Bratton, Sarah D. Eddy, Zofia Mazerska, Howard P. Hendrickson, Peter A. Crooks, Anna Radominska-Pandya
CHEMICAL RESEARCH IN TOXICOLOGY
(2014)
Article
Chemistry, Medicinal
Narsimha R. Penthala, Shobanbabu Bommagani, Venumadhav Janganati, Kenzie B. MacNicol, Chad E. Cragle, Nikhil R. Madadi, Linda L. Hardy, Angus M. MacNicol, Peter A. Crooks
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2014)
Article
Pharmacology & Pharmacy
Lirit N. Franks, Benjamin M. Ford, Nikhil R. Madadi, Narsimha R. Penthala, Peter A. Crooks, Paul L. Prather
EUROPEAN JOURNAL OF PHARMACOLOGY
(2014)
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)