Article
Biochemistry & Molecular Biology
Malgorzata Gora, Anna Czopek, Anna Rapacz, Anna Gebska, Katarzyna Wojcik-Pszczola, Elzbieta Pekala, Krzysztof Kaminski
Summary: A novel series of 3-(2-chlorophenyl)- and 3-(3-chlorophenyl)-pyrrolidine-2,5-dione-acetamide derivatives were synthesized and evaluated for their anticonvulsant and analgesic activities. The most active compound showed promising results in the acute models of epilepsy and tonic pain, with a potential mechanism of action involving interaction with neuronal voltage-sensitive sodium and L-type calcium channels. Additionally, the compounds exhibited no significant cytotoxic effects in neurotoxicity and hepatotoxicity assays.
Article
Chemistry, Multidisciplinary
Zhi-xu Zhou, Qing-mei Wu, Zhu-yan Huang, De-hou Yu, Hong-guang Lu
Summary: In this study, a novel compound was synthesized and characterized using various spectroscopic methods. Molecular docking analysis indicated potential interactions between the compound and SHP2 protein. In vitro experiments demonstrated promising antitumor activity of the compound.
RESEARCH ON CHEMICAL INTERMEDIATES
(2021)
Article
Chemistry, Physical
Seyedeh Mahdieh Hashemi, Saeed Emami, Patrick Honarchian Masihi, Aidin Shakiba, Leila Dehestani, Nematollah Ahangar
Summary: A series of novel 1-(2-(halophenyl)-2-(2-arylhydrazono)ethyl)-1H-1,2,4-triazoles 7a-l and their Fischer indolic products 2-(halophenyl)-3-(1H-1,2,4-triazol-1-yl)-1H-indoles 8a-l were synthesized conveniently. The (Z or E) geometry of arylhydrazones was identified by 1H NMR spectroscopy. The antiepileptic potential of both series of compounds was evaluated using PTZ and MES seizure models. The majority of hydrazones exhibited significant protective effects against MES-induced seizures, with compounds 7a and 7h being the most potent and rapid-acting. Indolic compounds generally displayed lower activity compared to their original arylhydrazones.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Aneta Pogorzelska, Jaroslaw Slawinski, Anna Kawiak, Grzegorz Stasilojc, Jaroslaw Chojnacki
Summary: The reaction between chalcones and benzenesulfonylaminoguanidines resulted in the synthesis of new guanidine derivatives. These compounds were tested for their impact on the growth of breast cancer cells MCF-7, cervical cancer cells HeLa, and colon cancer cells HCT-116. The presence of a hydroxy group in the benzene ring was found to strongly affect the activity of the derivatives. The most cytotoxic compounds displayed significant inhibitory effects on the tested cell lines, particularly against the malignant cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Jun Wu, Zhipeng Hou, Yan Wang, Liping Chen, Chengxi Lian, Qingfei Meng, Chaoying Zhang, Xiufen Li, Longjiang Huang, Haibo Yu
Summary: A series of 7-alkoxy -[1,2,4] triazolo [1, 5-a] pyrimidine derivatives were synthesized and found to exhibit significant anti-seizure effects. The compounds mainly exerted their anticonvulsant activity by allosteric potentiation of GABA(A) receptors. Compound 10c, with potent activity, showed sensitivity to different subunit configurations of GABA(A) receptors and acted on distinct sites from benzodiazepines and barbiturates. These structural compounds may serve as a foundation for designing novel antiepileptic molecules.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Jinxia Wen, Wenyan Zhao, Xu Gao, Xiaofang Ren, Chunping Dong, Cheli Wang, Li Liu, Jian Li
Summary: An efficient synthesis of various [1,2,3]triazolo-[1,5-a]quinoxalin-4(5H)-ones via [3 + 2] cyclization reaction by photoredox catalysis between quinoxalinones and hypervalent iodine(III) reagents is reported. A wide range of quinoxalinones and hypervalent iodine(III) reagents were well tolerated. This cyclization reaction allows the access to structurally diverse [1,2,3]triazolo-[1,5-a]quinoxalin-4(SH)-ones in moderate to good yields.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Physical
Qingmei Wu, Zhaopeng Zheng, Wenjun Ye, Qian Guo, Tianhui Liao, Di Yang, Chunshen Zhao, Weike Liao, Huifang Chai, Zhixu Zhou
Summary: In this study, a new compound was synthesized and characterized using spectroscopy, X-ray crystallography, and computational chemistry methods. The results demonstrated potential inhibitory activity of the compound on the SHP2 protein, suggesting promising applications in drug development.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Organic
Rungsima Hadsarung, Sanit Thongnest, Sittisak Oekchuae, Duangduan Chaiyaveij, Jutatip Boonsombat, Somsak Ruchirawat
Summary: This article describes an improved synthetic strategy for synthesizing 1-substituted 4-H phthalazines under mild conditions. The method has high practical value and can be used to synthesize various analogs.
Article
Materials Science, Multidisciplinary
L. Prodan, I. Filippova, A. O. Zubtsovskii, S. Shova, S. Widmann, A. A. Tsirlin, I. Kezsmarki, V. Tsurkan
Summary: We investigate the crystal structure, magnetization, and specific heat measurements of single crystals of the hexagonal polar magnet Co2-xZnxMo3O8. It is found that Zn doping can preserve the robust antiferromagnetic behavior in Co2Mo3O8 up to x = 0.55. The observed effects in the lattice parameter, Curie-Weiss temperature, and magnetic entropy can be attributed to the site-selective Zn substitution, which is dependent on the coordination of the Co2+ ions.
Article
Medicine, Research & Experimental
Szymon Jarzynski, Anna Rapacz, Anna Dziubina, Elzbieta Pekala, Justyna Popiol, Kamil Piska, Slawomir Wojtulewski, Bogna Rudolf
Summary: A series of 3-aminopyrrolidine-2,5-dione derivatives were synthesized and tested for anticonvulsant activity. The most active compound showed antiseizure activity in all seizure models, including pharmacoresistant seizures.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Biochemistry & Molecular Biology
Kamila Buzun, Anna Kryshchyshyn-Dylevych, Julia Senkiv, Olexandra Roman, Andrzej Gzella, Krzysztof Bielawski, Anna Bielawska, Roman Lesyk
Summary: A series of novel 5-[(Z,2Z)-2-chloro-3-(4-nitrophenyl)-2-propenylidene]-thiazolidinones were synthesized, with compound 2h showing the highest level of antimitotic activity against various cancer cell lines. Hit compounds were found to have low toxicity towards normal human blood lymphocytes and a fairly wide therapeutic range. The significance of specific substituents in the 4-thiazolidinone derivatives for anticancer cytotoxicity levels was established.
Article
Chemistry, Medicinal
Jolanta Obniska, Malgorzata Gora, Anna Rapacz, Kinga Salat, Sabina Rybka, Michal Abram, Marcin Jakubiec, Krzysztof Kaminski
Summary: A library of new compounds were synthesized and tested for anticonvulsant and analgesic activities, with one compound showing promising results in both aspects. The potential mechanism of action for this compound involves its influence on neuronal sodium and calcium channels.
ARCHIV DER PHARMAZIE
(2021)
Article
Medicine, Research & Experimental
Varsha Ananthapadmanabhan, Thomas C. Frost, Kara M. Soroko, Aine Knott, Brianna J. Magliozzi, Prafulla C. Gokhale, Vijaya G. Tirunagaru, Robert C. Doebele, James A. DeCaprio
Summary: In this study, the efficacy of milademetan, an MDM2 inhibitor, was assessed in various MCC models, showing significant inhibition on WT p53 MCC tumors. Useful in vitro and in vivo models for future MCC studies were also reported.
Article
Chemistry, Multidisciplinary
Mariia Nesterkina, Vladimir Musatov, Olena Honcharova, Iryna Kravchenko
Summary: Phenibut ester was synthesized using a coupling reagent and a catalyst, and its purity was assessed using various spectroscopic methods. The anticonvulsant profile of phenibut ester was examined in different seizure models.
Article
Oncology
Xin Chen, Zhichen Yu, Jianhua Wang, Wenjing Cui, Can Cui, Yajie Wang, Yongkang Liu, Hao Zhou, Cheng Wang, Zhongqiu Wang, Xiao Chen
Summary: The occurrence of PCLs is not uncommon in the Chinese general population, with location in the pancreatic head and extrapancreatic growth being independent predictors of high-risk PCLs and PCL progression.
CANCER MANAGEMENT AND RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Ali Mehri, Karim Mahnam, Hajar Sirous, Mahmoud Aghaei, Leila Rafiei, Mahboubeh Rostami
Summary: One potential approach for tumor therapy is inhibiting the binding between MDM2 and p53 to reactivate p53 in tumor cells. In this study, Monastrol derivatives were designed as MDM2 inhibitors and evaluated for their cytotoxicity on cancer cells. Compound 5d showed the best inhibitory results in silico and in vitro experiments. These findings suggest that Monastrol derivatives have the potential to be candidates for MDM2 inhibition.
CHEMICAL BIOLOGY & DRUG DESIGN
(2024)
