Article
Crystallography
Ahmed M. El-Agrody, Ahmed M. Fouda, Hany M. Mohamed, Mohammed Y. Alshahrani, Hazem A. Ghabbour, Abd El-Galil E. Amr, Rawda M. Okasha, Ahmed M. Naglah, Abdulrahman A. Almehizia, Ahmed A. Elhenawy
Summary: A target compound, 2-amino-4-(2,3-dichlorophenyl)-6-methoxy-4H-benzo[h]chromene-3-carbonitrile (4), was successfully synthesized and characterized. In vitro experiments demonstrated its strong and selective cytotoxicity against cancer cell lines. Promising inhibition efficacy was observed against EGFR and VEGFR-2 kinases.
Article
Chemistry, Physical
Faraz Ghous, Soni Shukla, Ramesh Singh, Shama Parveen, Monisha Banerjee, Abha Bishnoi
Summary: Since the discovery of cancer, both its mysterious origin and the mechanisms by which it spreads have baffled scientists. Targeted systemic chemotherapy with minimal side effects remains a future goal. A novel thiazolidin-4-one analogue was synthesized and experimentally investigated for its anti-lung cancer activity.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Multidisciplinary
Sha Zhu, Yerri Jagadeesh, Anh Tuan Tran, Shuki Imaeda, Alisdair Boraston, Dominic S. Alonzi, Ana Poveda, Yongmin Zhang, Jerome Desire, Julie Charollais-Thoenig, Stephane Demotz, Atsushi Kato, Terry D. Butters, Jesus Jimenez-Barbero, Matthieu Sollogoub, Yves Bleriot
Summary: In the study, a pharmacological chaperone approach was explored to enhance the activity of NAGLU in patient fibroblasts affected by Mucopolysaccharidosis type IIIB. By synthesizing a library of iminosugar C-glycosides, it was found that a non-functionalized and wrongly configured beta-homoiminosugar acted as the most promising pharmacological chaperone, promoting a 2.4 fold activity enhancement of mutant NAGLU at its optimal concentration.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Biochemistry & Molecular Biology
Yogita K. Abhale, Abhijit Shinde, Monika Shelke, Laxman Nawale, Dhiman Sarkar, Pravin C. Mhaske
Summary: A new series of 3-substituted phenyl-2-(2-(substituted phenyl)thiazol-4-yl) thiazolidin-4-one derivatives were synthesized and screened for antimycobacterial activity, with nine derivatives showing excellent activity against Mycobacterium bovis BCG. The compounds also exhibited low cytotoxicity against various cell lines, suggesting their potential for treating tuberculosis.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Organic
Amer A. Amer, Antar A. Abdelhamid, Amany Sh. Elnakeeb, Hanan A. Salah
Summary: An unprecedented series of 2-imino-1,3-thiazolidin-4-ones were designed using a straightforward and efficient method. The differences in the resulting products under different reaction conditions were also discovered.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Mojtaba Lashkari, Majid Ghashang
Summary: The hydrothermal synthesis of ZnO-NiO-NiFe(2)O(4)nanocomposite was characterized using various techniques. The nanocomposite showed superior catalytic activity in the synthesis of thiazolidin-4-one derivatives, outperforming individual metal oxides. Additionally, the catalyst could be recovered and reused multiple times.
RESEARCH ON CHEMICAL INTERMEDIATES
(2021)
Article
Chemistry, Physical
Deeksha Sharma, Saurabh Sharma, Niharika Sinha, Neha Jain, Amit Kumar, Anjana Sarkar, Jaya Sivaswami Tyagi, Rajesh Kumar Gupta
Summary: This study reported a high throughput screening assay to identify inhibitors that specifically target DevR and successfully discovered novel inhibitors. The interaction between these inhibitors and DevR was experimentally confirmed. These findings provide a new and promising scaffold for designing anti-DevR molecules to intercept mycobacterial dormancy.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Review
Chemistry, Medicinal
Nazar Trotsko
Summary: The thiazolidin-4-one scaffold is widely used in medicinal chemistry due to its broad biological activity, particularly in the field of anti-tuberculosis activity. Some compounds derived from this scaffold have shown promising anti-tuberculosis activity, outperforming reference drugs against various strains of Mycobacterium tuberculosis. The structure-activity relationship (SAR) and potential molecular targets of these compounds were also discussed in the review.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Helena Tuszewska, Jacek Szczepanski, Slawomir Mandziuk, Nazar Trotsko
Summary: Thiazolidin-4-one derivatives have potential as therapeutic agents for various protozoal infections, and this review focuses on their antitoxoplasmic, anti-trypanosomal, antimalarial, antileishmanial, and antiamoebic activities. The structure-activity relationship and main molecular targets of these derivatives are also discussed, providing useful information for the development of effective antiprotozoal agents.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Milan Kumar Mandal, Swagatika Ghosh, Lieve Naesens, Hans Raj Bhat, Udaya Pratap Singh
Summary: The study involved the synthesis of novel compounds with significant antimicrobial and antiviral activities, particularly showing strong inhibitory effects against bacteria and fungi, as well as considerable antiviral activity against various viruses. The findings suggest potential for the development of compounds with dual antimicrobial and antiviral properties.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Yanmei Luo, Jin Li, Yuliang Zong, Mengxin Sun, Wan Zheng, Jiapeng Zhu, Liu Liu, Bing Liu
Summary: This study identifies a potent SHP2 allosteric inhibitor and provides insights into its structure-activity relationship through comparison of co-crystal structures. These results have implications for understanding the mode of action and designing other allosteric inhibitors of SHP2.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Marina Ikegaya, Enoch Y. Park, Takatsugu Miyazaki
Summary: Glycoside hydrolase family 31 (GH31) contains a-glycoside hydrolases with different substrate specificities involved in various physiological functions. This study characterized two a-galactosidases, BsGH31_19 and FpGH31_19, and found that they showed high substrate specificity against a-(1?4)-linkages in a-(1?4)-galactobiose and globotriose, unlike other reported GH31 a-galactosidases PsGal31A and MYORG. Structural analyses revealed differences in amino acid residues and dimer interfaces between BsGH31_19 and FpGH31_19 compared to PsGal31A and MYORG, providing insights into the molecular diversity and evolutionary relationships of GH31 a-galactosidases and other a-galactosidase families.
Article
Chemistry, Multidisciplinary
Elena Calatrava-Perez, Luke A. Marchetti, Gavin J. McManus, Dylan M. Lynch, Robert B. P. Elmes, D. Clive Williams, Thorfinnur Gunnlaugsson, Eoin M. Scanlan
Summary: Real-time tracking of prodrug uptake, delivery and activation using novel glycosylated theranostics of the cancer pharmacophore Amonafide demonstrates highly-selective, enzymatic triggered release, preserving the potent cytotoxicity of Amonafide through targeted approach.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Chemistry, Applied
Ismail Althagafi, Nashwa El-Metwaly
Summary: Five novel co-sensitizers were synthesized and studied for their co-sensitization effect with standard Ru(II) dye (N-719) in dye-sensitized solar cells (DSSCs). Among them, IS-11 and IS-12 showed the highest power conversion efficiencies of 8.32% and 8.09%, respectively, when co-sensitized with N-719. This improved performance can be attributed to their maximum J(SC) values, indicating the importance of efficient co-sensitizers in enhancing DSSC performance.
APPLIED ORGANOMETALLIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Ioana Mirela Vasincu, Maria Apotrosoaei, Florentina Lupascu, Andreea-Teodora Iacob, Simona-Eliza Giusca, Irina-Draga Caruntu, Narcisa-Laura Marangoci, Anca Roxana Petrovici, Gabriela Dumitrita Stanciu, Bogdan-Ionel Tamba, Bianca-Stefania Profire, Alin-Viorel Focsa, Mariana Pinteala, Lenuta Profire
Summary: This study improves the solubility and stability of ibuprofen by forming β-CD complexes, reducing drug-related irritability and enhancing pharmacological and pharmacokinetics properties.
