Microwave assisted synthesis, characterization, molecular docking and pharmacological activities of some new 2′-hydroxychalcone derivatives
Publication date: 15 April 2020Source: Journal of Molecular Structure, Volume 1206Author(s): Mohammad Nasir Uddin, Md Nazmul Hassan Knock, Monir Uzzaman, M. Mosharef H. Bhuiyan, A.F.M. Sanaullah, Wahhida Shumi, Hossain Md Sadrul AminAbstractSynthesis of six new α, β-unsaturated carbonyl compounds (2′-hydroxychalcones) from 2′-hydroxyacethophenone and aromatic aldehyde derivatives under microwave condition has been described due to their pharmaceutical interest. They were characterized by FTIR, 1H NMR, Mass spectra, micro-analytical data and other physic-chemical properties. Density functional theory (DFT) with B3LYP/6-311 + G (d,p) has been employed for the optimization of all synthesized chalcones which helps to confirm the structures of the compounds proposed based on experimental evidences. The synthesized compounds were proved to inhibit microbial activity and showed good antioxidant property. Molecular docking was performed against prostaglandin H2 (PGH2) synthase protein 5F19. The binding affinity and binding mode of 2′-hydroxychalcones with this protein was searched considering paracetamol (PCT) as standard.Graphical abstract
Authors: Nieder C, Dalhaug A, Haukland E Abstract Aim: The aim of this study was to evaluate the feasibility and efficacy, in terms of overall survival, of sequential systemic therapy in patients with metastatic castration-resistant prostate cancer (MCRPC) who lived in Nordland County, Norway, a large region with a challenging geography, yet only one department of oncology located in the main city, Bodø.Patients and methods: Overall 77 patients who had received at least 2 lines of treatment were included in this retrospective study.Results: Management included docetaxel in 69 patients (90%), often prescribed...
Conclusion: Taken together, above results shown the protective effect of EPO on cyclosporine A-induced renal injury and confirmed that EPO's anti-inflammation and antioxidative stress involving the PPAR γ/TLR4/TGFβ1 axis. PMID: 32090669 [PubMed - in process]
Publication date: Available online 24 February 2020Source: The Lancet Respiratory MedicineAuthor(s): Jonathan Chun-Hei Cheung, Lap Tin Ho, Justin Vincent Cheng, Esther Yin Kwan Cham, Koon Ngai Lam
Publication date: Available online 24 February 2020Source: The Lancet Respiratory MedicineAuthor(s): Xiaobo Yang, Yuan Yu, Jiqian Xu, Huaqing Shu, Jia'an Xia, Hong Liu, Yongran Wu, Lu Zhang, Zhui Yu, Minghao Fang, Ting Yu, Yaxin Wang, Shangwen Pan, Xiaojing Zou, Shiying Yuan, You Shang
Publication date: Available online 24 February 2020Source: Respiratory InvestigationAuthor(s): Sze Shyang Kho, Swee Kim Chan, Mei Ching Yong, Hui Min Cheah, YC Gary Lee, Siew Teck Tie
Publication date: Available online 25 February 2020Source: Heart &LungAuthor(s): Patrick Lavoie, Sean P. Clarke, Christina Clausen, Margaret Purden, Jessica Emed, Tanya Mailhot, Guillaume Fontaine, Valerie Frunchak
Publication date: Available online 24 February 2020Source: Heart &LungAuthor(s): Prerna Gupta, Jennifer L. Martin, Dale M. Needham, Sitaram Vangala, Elizabeth Colantuoni, Biren B. Kamdar
Publication date: August 2020Source: Nonlinear Analysis: Real World Applications, Volume 54Author(s): Weimin Han
Szpakowska M Abstract Chemokines regulate directed cell migration, proliferation and survival and are key components in cancer biology. They exert their functions by interacting with seven-transmembrane domain receptors that signal through G proteins (GPCRs). A subgroup of four chemokine receptors known as the atypical chemokine receptors (ACKRs) has emerged as essential regulators of the chemokine functions. ACKRs play diverse and complex roles in tumor biology from tumor initiation to metastasis, including cancer cell proliferation, adherence to endothelium, epithelial-mesenchymal transition (EMT), extravasatio...
Abstract As basic research into GPCR signaling and its association with disease has come into fruition, greater clarity has emerged with regards to how these receptors may be amenable to therapeutic intervention. As a diverse group of receptor proteins, which regulate a variety of intracellular signaling pathways, research in this area has been slow to yield tangible therapeutic agents for the treatment of a number of diseases including cancer. However, recently such research has gained momentum based on a series of studies that have sought to define GPCR proteins dynamics through the elucidation of their crystal ...