Article
Chemistry, Medicinal
Laura Grau, Richard Soucek, M. Dolors Pujol
Summary: Resveratrol, a natural compound with antioxidant properties, has potential as both a chemopreventive and cancer chemotherapeutic agent. Due to its poor bioavailability, the study of new derivatives is important. In this study, (E)-stilbenes derived from resveratrol and cyclic analogues with benzofuran or indole nucleus were synthesized and evaluated for their impact on tumor growth. Some compounds showed higher cytotoxicity than (E)-resveratrol, with one derivative demonstrating eight times greater cytotoxic activity against colon cancer cells. Certain cyclic derivatives also exhibited strong inhibition of cell growth.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Jessica E. Mendieta-Wejebe, Martha C. Rosales-Hernandez, Itzia I. Padilla-Martinez, Efren V. Garcia-Baez, Alejandro Cruz
Summary: (T)Us and BTs have shown diverse biological activities. When combined, (T)UBTs are formed, which have improved physicochemical and biological properties, making them interesting for medicinal chemistry.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Chemistry, Multidisciplinary
Nadia A. A. Elkanzi, Hajer Hrichi, Ruba A. Alolayan, Wassila Derafa, Fatin M. Zahou, Rania B. Bakr
Summary: This review highlights the recent synthesis of chalcones bearing N, O, and/or S heterocycles and their biological potential. Literature review suggests that these chalcone-heterocycle hybrids show promise as future drug candidates with similar or superior activities compared to standards. This review is of significant importance for the development of new therapeutic drugs based on previously developed strategies.
Article
Multidisciplinary Sciences
Peipei Cui, Mingjiang Cai, Yanan Meng, Yan Yang, Hongjian Song, Yuxiu Liu, Qingmin Wang
Summary: In this study, a series of echinopsine derivatives containing acylhydrazone moieties were designed, synthesized, and evaluated for their biological activities. The compounds showed good antiviral activity against tobacco mosaic virus, as well as insecticidal and fungicidal activities.
SCIENTIFIC REPORTS
(2022)
Review
Biochemistry & Molecular Biology
Jianan Hu, Jirui Zhang, Jian He
Summary: Nonactic acid and its derivatives have attracted much attention due to their various biological activities, including antibacterial, insecticidal, acaricidal effects, and promoting plant growth. However, research on their anticancer activities is still limited.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Agriculture, Multidisciplinary
Lefeng Dong, Wenning Chang, Wulin Yang, Zhiping Xu, Jiagao Cheng, Xusheng Shao, Xiaoyong Xu, Zhong Li
Summary: 36 novel phenylpyrazole derivatives containing a trifluoromethylselenyl moiety were designed and synthesized, and their structures were characterized by NMR and HRMS. Some derivatives showed good insecticidal activities against Aedes albopictus and Plutella xylostella. Compounds 5 and 6 exhibited better insecticidal effects against Musca domestica.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Marie-Pierre Girard, Vahid Karimzadegan, Marianne Heneault, Francis Cloutier, Gervais Berube, Lionel Berthoux, Natacha Merindol, Isabel Desgagne-Penix
Summary: Amaryllidaceae alkaloids, particularly norbelladine and its derivatives, show therapeutic potential with antiviral and anticholinesterase properties. O-methylated norbelladine-type alkaloids possess inhibitory effects on DENV infection and butyrylcholinesterase.
Article
Plant Sciences
Xiao-Long Hu, Qi-Wei He, Huan Long, Li-Xin Zhang, Rong Wang, Bao-Lin Wang, Jia-Hao Feng, Quan Wang, Ji-Qin Hou, Xiao-Qi Zhang, Wen-Cai Ye, Hao Wang
Summary: In this study, 31 new celastrol derivatives were synthesized and evaluated for their ability to disrupt the Hsp90-Cdc37 interaction and inhibit cancer cell proliferation. Compound 4f showed the highest tumor cell selectivity, potent Hsp90-Cdc37 disruption activity, and antiproliferative effects, making it a promising candidate for the development of new cancer therapies. Further research demonstrated that 4f has strong antitumor activities in vitro and in vivo, with less toxicity compared to celastrol, suggesting its potential as a new cancer treatment option.
JOURNAL OF NATURAL PRODUCTS
(2021)
Article
Chemistry, Medicinal
Cangcang Xu, Linfan Xiao, Xia Zhang, Tao Zhuang, Lingli Mu, Xiaoping Yang
Summary: Novel artemisinin ester derivatives were synthesized and compound 2c showed the most potent anti-proliferative activity against OVCAR3 cells with low cytotoxicity, likely through targeting mitochondria and inducing cell apoptosis. These findings suggest compound 2c may be a promising candidate for further investigation against ovarian cancer.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Multidisciplinary
Pakkirisamy Sivakumar, Sarangapani Bharanidharan, Rajaram Rajamohan, Balasubramaniyan Anandhan, Thangavelu Sumathi, Subramaniyan Kamatchi
Summary: The design of organic molecules as drug molecules holds tremendous promise for success in both the present and future. Heterocyclic compounds, particularly 4-methylthiazole compounds (MTs), have been extensively studied and characterized using various techniques, revealing their potential as potent therapeutics for inflammation and diabetes treatment. The thorough examination includes analysis of molecular structures, determination of polarizability and first hyperpolarizability values, calculation of highest occupied and lowest unoccupied molecular orbital energies, investigation of molecular electrostatic potential, and evaluation of anti-inflammatory and anti-diabetic properties.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Ambar M. Alsina-Sanchez, Sebastian Montalvo-Vazquez, Nilmary Grafals-Ruiz, Carmen Acosta, Emily M. Orme, Israel Rodriguez, Sara M. Delgado-Rivera, Arthur D. Tinoco, Suranganie Dharmawardhane, Ingrid C. Montes-Gonzalez
Summary: Breast cancer is a common and dangerous disease, and finding effective treatments is crucial. In this study, novel ferrocenyl chalcones were synthesized and evaluated for their cytotoxicity against breast cancer cell lines. The compounds showed promising activity, especially those with five-membered heterocyclic substituents.
Article
Chemistry, Physical
Hima Bindhu Joolakanti, Ramanjaneyulu Kamepalli, Jeevanreddy Miryala, Satyanarayana Battu
Summary: The study identified a series of N-(3-((1H-1,2,3-triazol-4-yl)methoxy)phenyl)acetamide derivatives as potential compounds targeting Estrogen Receptor Alpha, with excellent bioactivity demonstrated in cell experiments.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Medicinal
Die Hu, Nian Zhang, Qing Zhou, Yuanxiang Zhou, Chenyu Gong, Yuanquan Zhang, Wei Xue
Summary: A series of novel chalcone derivatives containing pyrazole oxime ethers were designed and synthesized. The target compounds' structures were determined by NMR and HRMS, with H5 being confirmed via X-ray diffraction analysis. Some of the compounds showed significant antiviral and antibacterial activities. H9 exhibited the best curative and protective effect against tobacco mosaic virus, with superior binding ability to TMV-CP compared to ningnanmycin. H17 demonstrated good inhibiting effect against Xoo, with higher activity than thiodiazole copper and bismerthiazol, and its antibacterial activity was verified by SEM.
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
Biochemistry & Molecular Biology
Yuanyuan Zhang, Chuan Xie, Yang Liu, Feng Shang, Rushiya Shao, Jing Yu, Chunxia Wu, Xinghui Yao, Dongfang Liu, Zhouyu Wang
Summary: Antibiotic resistance is increasingly common and negatively impacts public health. Utilizing modifications of bioactive natural products in drug development can improve success rates, with a promising antibiotic candidate recently identified. Novel antibacterial compounds were synthesized and tested for their activity, showing potent effects against various strains, particularly MRSA, with potential for future use in combating drug-resistant bacteria.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Letter
Allergy
Katarzyna Molinska, Marta Latek, Blazej Rychlik, Jakub Lach, Dominik Strapagiel, Joanna Majak, Lukasz Blazowski, Joanna Jerzynska, Piotr Kuna, Pawel Majak
Article
Chemistry, Inorganic & Nuclear
Anna Wieczorek-Blauz, Karolina Kowalczyk, Andrzej Blauz, Anna Makal, Sylwia Pawledzio, Chatchakorn Eurtivong, Homayon J. Arabshahi, Johannes Reynisson, Christian G. Hartinger, Blazej Rychlik, Damian Plazuk
Summary: Incorporating the ferrocenyl moiety into a bioactive molecule can significantly alter the activity of the resulting conjugate. By applying this strategy, ferrocenyl analogs of monastrol were designed with higher antiproliferative activity and KSP modulatory activity, attributed to the presence of the ferrocenyl group.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Medicinal
Damian Kulaga, Anna K. Drabczyk, Grzegorz Satala, Gniewomir Latacz, Karolina Rozga, Damian Plazuk, Jolanta Jaskowska
Summary: Arylpiperazine derivatives with dual 5-HT1A/5-HT7 action are widely used for treating central nervous system diseases; two newly designed 5-HT7 ligands showed good metabolic stability and different hepatotoxicity performances.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Damian Kulaga, Anna Karolina Drabczyk, Grzegorz Satala, Gniewomir Latacz, Anna Boguszewska-Czubara, Damian Plazuk, Jolanta Jaskowska
Summary: In this study, novel 1,3,5-triazine derivatives were designed and synthesized as 5-HT7 receptor ligands. Two of the tested compounds showed high affinity and moderate metabolic stability, with low hepatotoxicity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Patryk Rybczynski, Anna Kaczmarek-Kedziera, Alex Iglesias-Reguant, Damian Plazuk, Borys Osmialowski
Summary: The tautomeric equilibrium of a series of 1-benzamidoisoquinoline derivatives was investigated using NMR spectroscopy and computational chemistry. The substitution effect could control the equilibrium between different tautomers, with the relative content of the amide form varying depending on the substituent. Unlike 2-phenacylquinoline derivatives, the most stable tautomer in the 1-benzamidoisoquinoline series was an amide, except for the two most electron-accepting substituents. The inclusion of explicit solvent was necessary to reproduce the experimental tendencies observed in this system, particularly for the formation of strong intermolecular hydrogen bonds.
Article
Chemistry, Multidisciplinary
Karolina Kowalczyk, Andrzej Blauz, Daniel Moscoh Ayine-Tora, Christian G. Hartinger, Blazej Rychlik, Damian Plazuk
Summary: Derivatives of ispinesib and its (S) analogue, containing ferrocenyl moieties or bulky organic substituents, were prepared to combine multiple biologically-active components in a single molecule. Several of these compounds demonstrated higher antiproliferative activity than ispinesib, with nanomolar IC50 values against cell lines. The improved activity may be attributed to synergic effects of various factors such as KSP inhibitory activity due to the ispinesib core and ability to generate ROS and induce mitotic arrest.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Applied
Marta Glodek, Elizaveta F. Petrusevich, Damian Plazuk, Denis Jacquemin, Borys Osmialowski
Summary: A series of difluoroborate fluorescent dyes with intramolecular charge transfer were synthesized and their properties were studied using both experimental and computational approaches. The size of the polyaromatic hydrocarbon side chains affects the photophysical properties of the dyes, especially their fluorescence quantum yield. Interestingly, corannulene, which is typically considered to lower the emission brightness, exhibited the highest fluorescence quantum yield in the series. Additionally, weak H/F or H/H intramolecular repulsions impacted the properties of BF2-carrying fluorophores.
Article
Optics
Mateusz Chorobinski, Paulina Smialek, Marta Gordel-Wojcik, Elizaveta F. Petrusevich, Eugeniusz Zych, Damian Plazuk, Lukasz Skowronski, Beata Jedrzejewska
Summary: The photophysical and optical properties of 4-(4'-(diphenylamino)benzylidene)-2-phenyloxazol-5(4H)-ones with different peripheral substituents were investigated in various environments. The nature of the substituent on the phenyl ring and the solvent mixture influenced these properties. The brightest emission was observed in solid state for the dye with a phenyl group or no substituent in the para position, while the dye with a cyano functional group showed the strongest emission in chloroform. The spectroscopic behavior of the dyes depended on the solvent mixture.
JOURNAL OF LUMINESCENCE
(2023)
Article
Pediatrics
Marta Latek, Piotr Lacwik, Katarzyna Molinska, Andrzej Blauz, Jakub Lach, Blazej Rychlik, Dominik Strapagiel, Joanna Majak, Joanna Molinska, Dorota Czech, Michal Seweryn, Piotr Kuna, Cezary Palczynski, Pawel Majak
Summary: This open-label randomized clinical trial demonstrated that treatment with intranasal corticosteroids improved the quality of life of children with chronic rhinosinusitis and had a significant effect on increasing sinonasal biodiversity. Although further investigation is needed, these data may reinforce the recommendation of using intranasal corticosteroids as a first-line treatment of chronic rhinosinusitis in children.
Article
Spectroscopy
Elizaveta F. Petrusevich, Marta Glodek, Magda A. Antoniak, Tadeusz Muziol, Damian Plazuk, Agnieszka Siomra, Marcin Nyk, Borys Osmialowski, Robert Zalesny
Summary: In this study, the symmetry relaxation effects on one- and two-photon absorption spectra of two bichromophore systems were investigated. The results showed that the planarity and deviations from planarity of the biphenyl moiety affected the two-photon transition strengths. Additionally, the perpendicular arrangement of phenylene units in the biphenylene moiety led to a decrease in two-photon transition strengths. The difference in two-photon absorption cross section between the two compounds was attributed to differences in equilibrium geometry.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2023)
