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Front Med (Lausanne) 2021 23;8:556776. Epub 2021 Mar 23.

Department of Infectious Diseases, West German Centre of Infectious Diseases, University Duisburg-Essen, Essen, Germany.

Cytotoxic CD8 T-cells play a pivotal role in the pathogenesis of systemic lupus erythematosus (SLE). The aim of this study was to investigate the role of CD107a (LAMP-1) on cytotoxic CD8 T-cells in SLE-patients in particular with lupus nephritis. Peripheral blood of SLE-patients ( = 31) and healthy controls ( = 21) was analyzed for the expression of CD314 and CD107a by flow cytometry. Read More

Drug Des Devel Ther 2021 1;15:1459-1476. Epub 2021 Apr 1.

State Key Laboratory of Oncogenomics, School of Chemical Biology and Biotechnology, Shenzhen Graduate School, Peking University, Shenzhen, People's Republic of China.

Purpose: The development of resistance to available anticancer drugs is increasingly becoming a major challenge and new chemical entities could be unveiled to compensate this therapeutic failure. The current study demonstrated the synthesis of 2-aminothiazole [() and ()] and 2-aminopyridine [() and ()] derivatives that can target multiple cellular networks implicated in cancer development.

Methods: Biological assays were performed to investigate the antioxidant and anticancer potential of synthesized compounds. Read More

J Inorg Biochem 2021 Mar 19;219:111425. Epub 2021 Mar 19.

Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Engineering and Technology Research Center of Characteristic Chinese Medicine Modernization, College of Pharmacy, Ningxia Medical University, Yinchuan 750004, PR China. Electronic address:

A series of tripodal ferrocenyl bis-naphthalimide derivatives were synthesized and characterized. All of the bis-naphthalimide derivatives exhibited good DNA binding ability which was confirmed by ethidium bromide (EB) displacement experiment and ultraviolet (UV)-visible absorption titration. And the binding mode of these compounds was proved to be a hybrid binding mode by experiments. Read More

Bioorg Chem 2021 Mar 17;112:104831. Epub 2021 Mar 17.

Department of Chemistry, Faculty of Science, Silpakorn University, Nakhon Pathom 73000, Thailand. Electronic address:

A series of 1,2,3-triazole-containing Sorafenib analogues, in which the aryl urea moiety of Sorafenib (1) was replaced with a 1,2,3-triazole ring linking a substituted phenoxy fragment, were prepared successfully via Huisgen 1,3-dipolar cycloaddition and nucleophilic aromatic substitution. The studies of cytotoxicity towards human hepatocellular carcinoma (HCC) cell lines, HepG2 and Huh7, indicated that p-tert-butylphenoxy analogue 2m showed significant inhibitory activity against Huh7 with IC = 5.67 ± 0. Read More

Parasitol Int 2021 Apr 5:102342. Epub 2021 Apr 5.

Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, Seropédica, RJ, Brazil. Electronic address:

Leishmaniasis is a neglected broad clinical spectrum disease caused by protozoa of the genus Leishmania, which affect millions of people annually in the world and the treatment has severe side effects and resistant strains have been reported. Mesoionic salts are a subclass of the betaine group with extensive biological activity such as microbicide and anti-inflammatory In this work, we analyze the cytotoxic effects of mesoionic salts, 4-phenyl-5-(X-phenyl)-1,3,4-thiadiazolium-2-phenylamine chloride (X = 4-Cl; 3, 4-diCl and 3,4-diF), on Leishmania amazonensis in vitro. Initially, Mesoionic salts toxicity were evaluated by XTT assay on L. Read More