Article
Chemistry, Physical
Saadat Hajari, Hassan Keypour, Mohammad Taher Rezaei, Seyed Hamed Moazzami Farida, Robert William Gable
Summary: In this study, 15-membered-ring symmetrical pentaaza macrocyclic Schiff base complexes were prepared using a template approach, and characterized using various techniques. The complexes showed strong antioxidant activity and moderate bactericidal activity, as well as significant cytotoxicity against breast and lung adenocarcinoma cells. Comparatively, [ZnLBr]ClO4 exhibited greater cytotoxic effect against the tested cells.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Leonardo S. A. Carneiro, Fernando Almeida-Souza, Yanne S. C. Lopes, Rachel C. Novas, Kaique B. A. Santos, Carolina B. P. Ligiero, Katia da S. Calabrese, Camilla D. Buarque
Summary: The new series of compounds showed promising activity against Leishmania parasites in vitro, with compound 17x identified as a potential candidate for anti-leishmaniasis drugs.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Organic
Marie Pascaline Rahelivao, Ingmar Bauer, Tilo Luebken, Olga Kataeva, Anne Vehlow, Nils Cordes, Hans-Joachim Knoelker
Summary: The relative configuration of the marine sesquiterpenoid oxyfungiformin, isolated from the soft coral Capnella fungiformis, was confirmed by synthesis and comparison of values for optical rotation. The cytotoxic activity of oxyfungiformin and a diastereoisomer was observed in lung, breast, and cervical cancer cells.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Physical
Irfan Sahin, Fatma Betul Ozgeris, Muhammet Kose, Ebubekir Bakan, Ferhan Tumer
Summary: This study synthesized six 1,2,3-triazole derivatives and investigated their antioxidant and anticancer activities. The results showed that some of the compounds exhibited significant anticancer activity.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Multidisciplinary Sciences
Mariam T. Sayed, Salwa A. Elsharabasy, Anhar Abdel-Aziem
Summary: Microbial infections are currently a widespread disease in hospitals and community health centres and are a major cause of death worldwide. Coumarin linked to thiazoles, pyridines and pyrazoles have been developed and evaluated for their antimicrobial properties against different microorganisms. Some of the prepared coumarins displayed high to moderate activity against the tested microorganisms with respect to the reference drugs, and compound 3 showed equal antimicrobial effect as Ciprofloxacin for Enterobacter cloacae. Compound 12 exhibited the most potent activity against Bacillus pumilis, while compounds 3, 4, and 12 showed remarkable activity against Streptococcus faecalis.
SCIENTIFIC REPORTS
(2023)
Article
Chemistry, Inorganic & Nuclear
Yordan Stremski, Maria Bachvarova, Stela Statkova-Abeghe, Plamen Angelov, Iliyan Ivanov, Anife Ahmedova, Anna Dolega
Summary: Novel ferrocenyl-containing benzothiazole derivatives were synthesized in moderate yields by one-pot alpha-amidoalkylation of ferrocene. The obtained compounds were further oxidized to known fully aromatic 2-ferrocenylbenzothiazole in high yield, offering a convenient alternative to previous methods.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Jaspreet S. Dhau, Avtar Singh, Paula Brandao, Vitor Felix
Summary: A new methodology for synthesizing bis[3-(4-chloro-N,N-diethylpyridine-2-carboxamide)] diselenide has been successfully achieved, characterized by various spectroscopic techniques and X-ray diffraction analysis. The compound showed antibacterial activity, with comparisons made to other pyridylselenium compounds and the standard drug Ampicillin.
INORGANIC CHEMISTRY COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Marian N. Aziz, Arzoo Patel, Amany Iskander, Avisankar Chini, Delphine Gout, Subhrangsu S. Mandal, Carl J. Lovely
Summary: An efficient surface-mediated synthetic method was developed to access a novel class of thiazolidines. These synthesized compounds showed potent anti-proliferative activity against a breast cancer cell line, MCF7, with higher activity compared to the standard reference, cisplatin.
Article
Biochemistry & Molecular Biology
Denis Sudarikov, Yulia Gyrdymova, Alexander Borisov, Julia M. Lukiyanova, Roman Rumyantcev, Oksana G. Shevchenko, Diana R. Baidamshina, Nargiza D. Zakarova, Airat R. Kayumov, Ekaterina O. Sinegubova, Alexandrina S. Volobueva, Vladimir V. Zarubaev, Svetlana A. Rubtsova
Summary: New unsymmetrical monoterpenylhetaryl disulfides based on heterocyclic disulfides and monoterpene thiols were synthesized for the first time. The compounds were evaluated for antioxidant, antibacterial, antifungal activity, cytotoxicity and mutagenicity.
Article
Chemistry, Physical
S. Naveen, Karthik Kumara, A. Dileep Kumar, K. Ajay Kumar, Abdelkader Zarrouk, Ismail Warad, N. K. Lokanath
Summary: The study presented an effective route for the direct synthesis of substituted pyrazole through 3+2 annulation method, with detailed characterization and analysis methods for the synthesized product. The compound was evaluated for antioxidant susceptibilities through DPPH and hydroxyl radical scavenging methods, showing promising results. The optimized theoretical structure parameters were in good agreement with the experimentally analyzed data, confirming the reliability of the synthesized compound.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
Orsolya Domotor, Ricardo G. Teixeira, Gabriella Spengler, Fernando Avecilla, Fernanda Marques, Oscar A. Lenis-Rojas, Cristina P. Matos, Rodrigo F. M. de Almeida, Eva A. Enyedy, Ana Isabel Tomaz
Summary: In this study, two Ru(II)-polypyridyl compounds were prepared and characterized. The solid-state structure was confirmed by X-ray diffraction analysis. The solubility, stability, and lipophilicity of the complexes were investigated under physiological mimetic conditions, as well as their potential uptake by passive diffusion. The complexes exhibited cytotoxicity on ovarian and colon cancer cells and induced late apoptosis and necrosis. They showed weak binding to human serum albumin but significant binding to calf thymus DNA.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Chemistry, Medicinal
Adam A. A. Sulaiman, Naike Casagrande, Cinzia Borghese, Giuseppe Corona, Anvarhusein A. Isab, Saeed Ahmad, Donatella Aldinucci, Muhammad Altaf
Summary: A new series of gold(I) complexes were synthesized and evaluated for their antitumor activity in ovarian cancer models. Complex 6 exhibited the highest antiproliferative effect and demonstrated anticancer activity in both in vitro and in vivo models. These results suggest the potential use of these complexes in future clinical applications.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Sunil L. Dhonnar, Rahul A. More, Vishnu A. Adole, Bapu S. Jagdale, Nutan Sadgir, Santosh S. Chobe
Summary: A series of 1,3,4-oxadiazole derivatives were synthesized and characterized. The synthesized compounds exhibited significant antibacterial and antifungal activity, as well as good antioxidant properties and low cytotoxicity. Three compounds showed higher antibacterial activity.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Inorganic & Nuclear
Songul Eglence-Bakir, Musa Sahin, Mustafa Ozyurek, Bahri Ulkuseven
Summary: Eight dioxomolybdenum(VI) complexes of 4-benzyloxysalicylidene N- or S-alkyl substituted thiosemicarbazones were synthesized and characterized, with one crystal structure being determined. The total antioxidant capacities were measured using the CUPRAC method, showing higher TEAC values for ONN series compared to ONS series. Scavenging effects for hydroxyl radical and xanthine oxidase inhibition activities were also investigated.
Article
Crystallography
Mezna Saleh Altowyan, Mostafa A. El-Naggar, Morsy A. M. Abu-Youssef, Saied M. Soliman, Matti Haukka, Assem Barakat, Ahmed M. A. Badr
Summary: A novel Ag(I) citrate complex with ethyl-3-quinolate (Et3qu) was synthesized and characterized. The complex exhibited broad-spectrum antimicrobial activity against A. fumigatus and demonstrated potent anticancer activity against breast and lung cancer cell lines.
Article
Chemistry, Medicinal
Zeynep Demir, Ebru Bilget Guven, Suheyla Ozbey, Canan Kazak, Rengul Cetin Atalay, Meral Tuncbilek
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Organic
Ozlen Guzel-Akdemir, Atilla Akdemir, Nilgun Karali, Claudiu T. Supuran
ORGANIC & BIOMOLECULAR CHEMISTRY
(2015)
Meeting Abstract
Chemistry, Multidisciplinary
Arzu Karayel, F. Betul Kayanak, Nilgun Karali, Suheyla Ozbey
ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES
(2015)
Meeting Abstract
Chemistry, Multidisciplinary
Suheyla Ozbey, Damla Kocak, Filiz Betul Kaynak, Figen Caliskan
ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES
(2015)
Article
Biochemistry & Molecular Biology
Atilla Akdemir, Ozlen Guzel-Akdemir, Nilgun Karali, Claudiu T. Supuran
BIOORGANIC & MEDICINAL CHEMISTRY
(2016)
Meeting Abstract
Chemistry, Multidisciplinary
Filiz B. Kaynak, Gulsum Gundogdu, Melanie Muller, Suheyla Ozbey
ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES
(2016)
Article
Biochemistry & Molecular Biology
Ozlen Guzel-Akdemir, Andrea Angeli, Kubra Demir, Claudiu T. Supuran, Atilla Akdemir
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2018)
Article
Biochemistry & Molecular Biology
Atilla Akdemir, Andrea Angeli, Fuesun Goektas, Pinar Eraslan Elma, Nilguen Karali, Claudiu T. Supuran
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2019)
Article
Biochemistry & Molecular Biology
Kubra Demir-Yazici, Silvia Bua, Nurgul Mutlu Akgunes, Atilla Akdemir, Claudiu T. Supuran, Ozlen Guzel-Akdemir
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2019)
Article
Biochemistry & Molecular Biology
OEzlen Guezel-Akdemir, Simone Carradori, Rossella Grande, Kuebra Demir-Yazici, Andrea Angeli, Claudiu T. Supuran, Atilla Akdemir
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2020)
Article
Pharmacology & Pharmacy
Efe Donukan Dincel, Dilek Satana, Suheyla Ozbey, Nuray Ulusoy-Guzeldemirci
Summary: A series of novel compounds were designed and synthesized in this study. The structures of these compounds were elucidated using various analytical methods. The results showed that compounds 2f, 3, and 5c exhibited antimycobacterial activity, and compound 2b displayed antifungal activity against T. rubrum. Based on these findings, compounds 2f, 3, and 5c are promising structures for future drug development.
JOURNAL OF RESEARCH IN PHARMACY
(2022)
Article
Biochemistry & Molecular Biology
Zekiye Seyma Sevincli, Gizem Nur Duran, Mehmet Ozbil, Nilgun Karali
BIOORGANIC CHEMISTRY
(2020)
Article
Pharmacology & Pharmacy
Gokce Cihan-Ustundag, Nurten Ozsoy, Ezgi Oztas, Nilgun Karali, Gultaze Capan
MARMARA PHARMACEUTICAL JOURNAL
(2017)
Article
Biochemistry & Molecular Biology
Nilgun Karali, Atilla Akdemir, Fusun Goktas, Pinar Eraslan Elma, Andrea Angeli, Merih Kizilirmak, Claudiu T. Supuran
BIOORGANIC & MEDICINAL CHEMISTRY
(2017)
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)