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Sulphonyl thiourea compounds containing pyrimidine as dual inhibitors of I, II, IX, and XII carbonic anhydrases and cancer cell lines: synthesis, characterization and studies.
RSC Med Chem
December 2024
VNU University of Education, Vietnam National University, Hanoi 144 Xuan Thuy, Cau Giay Ha Noi Vietnam.
Some novel sulphonyl thiourea derivatives (7a-m) containing 4,6-diarylpyrimidine rings were designed and synthesized using a one-pot procedure. These compounds exhibited remarkable dual inhibitory activity against human carbonic anhydrase CA I, CA II, CA IX, and XII isoenzymes and some cancer cell lines. Among them, some thioureas had significantly more potent inhibitory activities in the order of 7l > 7c > 7f (against the CA I isoform), 7f > 7b > 7c (against the CA II isoform), 7c > 7g > 7a > 7b (against the CA IX isoform), and 7d > 7c > 7g > 7f (against the CA XII isoform).
View Article and Find Full Text PDF[Clinical observation and anti-drug antibody monitoring of enzyme replacement therapy in children with Fabry disease].
Zhonghua Er Ke Za Zhi
January 2025
Department of Nephrology, Children's Hospital, Zhejiang University School of Medicine, National Clinical Research Center for Child Health, Hangzhou310052, China.
To analyze the efficacy of enzyme replacement therapy and anti-drug antibody production in children with Fabry disease. The clinical data of 7 children with Fabry disease treated with enzyme replacement therapy for more than 1 year at Children's Hospital of Zhejiang University School of Medicine from July 2021 to June 2024 were retrospectively analyzed. The basic information and the changes of related clinical indicators before and after treatment were collected.
View Article and Find Full Text PDFAnticancer and Cyclooxygenase Inhibitory Activity of Benzylidene Derivatives of Fenobam and its Thio Analogues.
Curr Med Chem
December 2024
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
Introduction: A series of benzylidene derivatives of fenobam and its thio analogues (1-22) have been evaluated for their cytotoxicity against breast cancer (MCF-7, MDA-MB-231), ovarian cancer (A2780, SKOV-3) and cervical cancer (HELA) cell lines.
Method: These compounds (1-22) exhibited 72-83% inhibition of Erk activity against the ovarian cancer cell line (A2780). Compounds 3 and 20 showed the highest DNA damage effect in Comet Assay against the A2780 cancer cell line as compared to the other tested analogues (4, 8, 11, 12, and 13) by using % Tail DNA and OTM.
In Vitro and Computational Response of Differential Catalysis by BAFC 633 Laccase in Interaction with 2,4-D and Chlorpyrifos.
Int J Mol Sci
November 2024
Laboratorio de Biotecnología Molecular, Instituto de Biotecnología de Misiones "Dra. Maria Ebe Reca" (InBioMis), Facultad de Ciencias Exactas Químicas y Naturales, Universidad Nacional de Misiones, Posadas 3300, Misiones, Argentina.
Enzymes secreted by white rot fungi (WRF), such as laccase, offer a promising approach for the treatment of hazardous xenobiotic compounds. This study conducted a comprehensive analysis of the impact of the pesticides 2,4-dichlorophenoxyacetic acid (2,4-D) and chlorpyrifos on the laccase of BAFC 633 through in vitro and bioinformatics analyses. The fungal strain was shown to be tolerant to both pesticides, with notable morphological and ultrastructural alterations in the mycelium.
View Article and Find Full Text PDFNovel Dibenzoazepine-Substituted Triazole Hybrids as Cholinesterase and Carbonic Anhydrase Inhibitors and Anticancer Agents: Synthesis, Characterization, Biological Evaluation, and Studies.
ACS Omega
November 2024
Department of Medical Biology, Faculty of Medicine, Çanakkale Onsekiz Mart University, 17020 Çanakkale, Türkiye.
The new dibenzoazepine-substituted triazole hybrids (-) were designed by molecular hybridization approach and synthesized utilizing the Cu(I)-catalyzed click reaction. The hybrid structures (-) were obtained in high yields (74-98%) with a simple two-step synthesis strategy and fully characterized. These compounds were assessed for their influence on various metabolic enzymes including human carbonic anhydrase isoenzymes (hCA I and hCA II), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE).
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