Review
Biochemistry & Molecular Biology
Reihane Ghomashi, Shakila Ghomashi, Hamidreza Aghaei, Ahmad Reza Massah
Summary: Sulfonamides are a diverse class of drugs with various pharmacological activities, including antibacterial, anti-carbonic anhydrase, anti-obesity, diuretic, hypoglycemic, antithyroid, antitumor, and anti-neuropathic pain activities. This review focuses on the recent advances in designing and developing two-component sulfonamide hybrids containing coumarin, indole, quinoline, isoquinoline, chalcone, pyrazole/pyrazoline, quinazoline, pyrimidine, thiazole, benzothiazole, and pyridine between 2015 and 2020. The synthesis and biological activity of these hybrid agents are comprehensively discussed.
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Organic
Zhi-You Huang, Ning Zhang, Han-Wen Zuo, Xu-Qi Zeng, Han Liu
Summary: A series of quinoline-6-sulfonamide compounds were designed based on the principle of active substructure splicing with ABA mimic and pyrabactin as lead compounds. These compounds could inhibit soybean seed germination and hold potential for discovering novel and highly active ABA functional mimics.
CHINESE JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Bonani Vinindwa, Godwin Akpeko Dziwornu, Wayiza Masamba
Summary: Molecular hybridization is a drug discovery strategy involving the fusion of two or more drugs to create new compounds with improved efficacy and reduced side effects. This approach aims to enhance the affinity and therapeutic effects of the parent drugs through rational design.
Article
Chemistry, Physical
Manal M. Khowdiary, Nahla A. Taha, Nashwa M. Saleh, Ahmed A. Elhenawy
Summary: Novel corrosion inhibitors and biocide metal complex nanoparticle surfactants were synthesized and evaluated for their performance in solution. The results showed excellent corrosion inhibition and antibacterial activity.
Article
Biochemistry & Molecular Biology
Xiangpan Li, Qing Chen, Jingsheng Ao, Wenxin Lin, Liqin Qiu, Rihui Cao
Summary: A series of new 4,7-disubstituted quinoline derivatives were designed, synthesized, and evaluated for their antiproliferative activity. Compound 10k showed the most potent antiproliferative activity and inhibited colorectal cancer growth through inducing autophagy.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Zhen-Feng Wang, Xiao-Ling Nai, Yue Xu, Feng-Hua Pan, Fu-Shun Tang, Qi-Pin Qin, Lin Yang, Shu-Hua Zhang
Summary: Four novel rhodium(iii) complexes were synthesized and found to exhibit selective cytotoxicity against cisplatin-resistant lung carcinoma cells. One of the complexes, a fluorescent imaging agent, showed high anticancer activity in the cell nucleus.
DALTON TRANSACTIONS
(2022)
Review
Chemistry, Multidisciplinary
Chao Wang, Jing Chang, Shanbo Yang, Lingyu Shi, Yujing Zhang, Wenjing Liu, Jingsen Meng, Jun Zeng, Renshuai Zhang, Dongming Xing
Summary: This article reviews the research progress of novel CA-4 containing quinoline analogs in anti-tumor from 1992 to 2022 and expounds on the pharmacological mechanisms of these effective compounds, including but not limited to apoptosis, cell cycle, tubulin polymerization inhibition, immune Fluorescence experiments, etc., which lay the foundation for the subsequent development of CA-4 containing quinoline analogs for clinical use.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Subhasis Dey, Anjali Patel, Nandan Haloi, Soumya Srimayee, Suman Paul, Ganesh Kumar Barik, Nasim Akhtar, Dipanjan Shaw, Gunanka Hazarika, Biswa Mohan Prusty, Mohit Kumar, Manas Kumar Santra, Emad Tajkhorshid, Surajit Bhattacharjee, Debasis Manna
Summary: This study reports the development of a new 8-aminoquinoline derivative with promising antibacterial activity against Gram-positive bacteria, reduced hemolytic activity and cytotoxicity to mammalian cells. In addition, the combination of this derivative showed excellent efficacy against Staphylococcus aureus and restored the susceptibility of other antibiotics against drug-resistant bacterial strains. The findings suggest that transmembrane zinc ion transport by the derivative could be a promising strategy for combating bacterial infections and restoring antibiotic activity.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Mohamed Helmy Abdelhameed Soliman, Ibrahim Ahmed Ibrahim Ali, Sahar Said Ahmed El-Sakka, Omayma El-Sayed Abdel-Basset Mohamed
Summary: New quinoline derivatives based on allyl and amino acid were synthesized and characterized, and their binding ability with HepG2 protein as well as their in vitro cytotoxic activity against hepatic carcinoma cells were evaluated. Among the synthesized compounds, compound 15d showed the most promising profile in inhibiting HepG2.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Multidisciplinary
A. O. Severin, S. G. Pilyo, L. M. Potikha, V. S. Brovarets
Summary: A method for synthesizing 5-phenyl-1,3-thiazole-4-sulfonyl chloride was developed using ethyl 2-{[1-(benzylsulfanyl)-2-oxo-2-phenylethyl]amino}-2-oxoacetate as an intermediate obtained from available reagents and through oxidative chlorination of benzyl 5-phenyl-1,3-thiazol-4-ylsulfide. The resulting compound was further converted into a series of 5-phenyl-1,3-thiazole-4-sulfonamide derivatives, which were then screened for in vitro antitumor activity on 60 cancer cell lines.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Myriam Gonzalez, Maria Ovejero-Sanchez, Alba Vicente-Blazquez, Raquel Alvarez, Ana B. Herrero, Manuel Medarde, Rogelio Gonzalez-Sarmiento, Rafael Pelaez
Summary: Pan-Gyn cancers represent 1 in 5 cancer cases worldwide, with breast cancer being the most common and deadliest among women. Due to the limitations of taxanes as first-line treatments, the development of alternative therapeutics has become urgent to combat these malignancies. Proposed alternatives targeting tubulin with compounds directed to the colchicine site show promising antiproliferative potencies and may offer a solution to chemoresistant Pan-Gyn cancers.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Xiaoyu Zhang, Guochuang Zheng, Shang Gao, Feng Zhou, Tao Pan, Qiqi Shi, Jiani Li, Xiaomeng Zhang, Zhangjian Huang, Xu Quan
Summary: In this study, phenyl sulfonamide was introduced to a series of 1H-pyrrolo[2,3-b]pyridine-2-carboxamide derivatives to obtain novel RSK2 inhibitors. The compounds showed strong RSK2 enzyme inhibitory activity and exhibited anti-proliferation activity against MDA-MB-468 cells. The newly introduced sulfonamide group formed a hydrogen bond with the target residue LEU-74, which played a crucial role in the activity.
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Article
Biochemistry & Molecular Biology
Moataz A. Shaldam, Hadia Almahli, Andrea Angeli, Rehab Mustafa Badi, Eman F. Khaleel, Abdelrahman I. Zain-Alabdeen, Zainab M. Elsayed, Eslam B. Elkaeed, Rofaida Salem, Claudiu T. Supuran, Wagdy M. Eldehna, Haytham O. Tawfik
Summary: New isatin-based sulphonamides were synthesized as potential dual VEGFR-2 and carbonic anhydrase inhibitors with anticancer activities. The most potent derivatives showed strong VEGFR-2 inhibitory effect but failed to inhibit relevant CA isoforms. Two derivatives were further tested for their impact on cell cycle disturbance and apoptotic potential. Molecular modelling analyses were conducted to assess the binding mode and stability of the target compounds.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Applied
Gaber A. El-Inany, Hussein S. Seleem, Basheir A. El-Shetary, Hoda F. El-Shafiy, Asmaa I. Nabeel, Aml Madyan, Magdy Shebl
Summary: A new hydrazone ligand (AlloxHQ) was obtained by reacting 1-(4-methylquinoline-2-yl)hydrazine with Alloxan. Binary copper (II) AlloxHQ complexes were successfully prepared using different copper (II) salts (chloride, bromide, sulfate, and acetate). Ternary complexes were also prepared using secondary ligands; 1,10-phenanthroline and oxine. The structures of AlloxHQ and Cu (II)-AlloxHQ complexes were investigated and their biological activity was confirmed through molecular docking studies.
APPLIED ORGANOMETALLIC CHEMISTRY
(2023)
Article
Plant Sciences
Pedro Martin-Acosta, Irene Cuadrado, Laura Gonzalez-Cofrade, Roberto Pestano, Sonsoles Hortelano, Beatriz de las Heras, Ana Estevez-Braun
Summary: A set of new dihydroquinoline embelin derivatives were synthesized from the reaction of natural benzoquinone embelin with anilines and aromatic aldehydes in the presence of AgOTf. The resulting compounds showed potential as cardioprotective agents, attenuating the cardiotoxicity effect of doxorubicin on oxidative stress and apoptosis. The best activities were achieved with quinoline-embelin derivatives having a 4-nitrophenyl group attached at the pyridine ring.
JOURNAL OF NATURAL PRODUCTS
(2023)
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)