6-Oxo and 6-thio analogs of purine were prepared based on the initial activity screening of a small, diverse purine library against Mycobacterium tuberculosis (Mtb). Certain 6-oxo and 6-thio-substituted purine analogs described herein showed moderate to good inhibitory activity. N(9)-substitution apparently enhances the anti-mycobacterial activity in the purine series described herein. Several 2-amino and 2-chloro purine analogs were also synthesized that showed moderate inhibitory activity against Mtb.
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http://dx.doi.org/10.1016/j.bmc.2013.01.054 | DOI Listing |
Sci Rep
January 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Debrecen, Egyetem tér 1, Debrecen, 4032, Hungary.
Hydrogen sulfide (HS) is an endogenous gasotransmitter with cardioprotective and antiviral effects. In this work, new cysteine-selective nucleoside-HS-donor hybrid molecules were prepared by conjugating nucleoside biomolecules with a thiol-activatable dithioacetyl group. 5'-Dithioacetate derivatives were synthesized from the canonical nucleosides (uridine, adenosine, cytidine, guanosine and thymidine), and the putative 5'-thio metabolites were also produced from uridine and adenosine.
View Article and Find Full Text PDFClin Exp Metastasis
January 2025
Department of Gastroenterology, The Second Affiliated Hospital of Zhejiang University School of Medicine, No.88, Jiefang Road, Hangzhou, 310009, Zhejiang, China.
Background: In recent years, the emphasis has shifted to understanding the role of N1-methyladenosine (m1A) in tumor progression as little is known about its regulatory effect on mRNA and its role in the metastasis of colorectal cancer (CRC).
Methods: We performed methylated RNA immunoprecipitation sequencing of tumor tissues and tumor-adjacent normal tissues from three patients with CRC to determine the m1A profile of mRNA in CRC. The expression of diaphanous-related formin 3 (DIAPH3) and its correlation with clinicopathological characteristics of CRC were evaluated using immunohistochemistry and online datasets.
Neurochem Res
January 2025
Dept Intens Care Unit, Hangzhou TCM Hospital Affiliated to Zhejiang Chinese Medical University, No.453, Stadium Road, Hangzhou, Zhejiang, 310007, China.
Glioblastoma (GBM) is the most malignant type of glioma with a very poor prognosis. N6-methyladenosine (m6A) is well-documented to be involved in GBM progression, and FTO is a demethylase. GSTO1 is also associated with tumor progression.
View Article and Find Full Text PDFUnderstanding the heterogeneity of epigenetic modifications within single cells is pivotal for unraveling the nature of the complexity of gene expression and cellular function. In this study, we have developed a strategy based on multichrome encoding and "AND" Boolean logic recognition for multiplexed, spatially resolved imaging of single-cell RNA epigenetic modifications, termed as PRoximity Exchange-assisted Encoding of Multichrome (PREEM). Through the implementation of this strategy, we can now map the expression and nuclear distribution of multiple site-specific RNA N6-methyladenosine (mA) modifications at the single-molecule resolution level in single-cells, and reveal the previously unknown heterogeneity.
View Article and Find Full Text PDFHua Xi Kou Qiang Yi Xue Za Zhi
February 2025
Dept. of Cariology and Endodontics, Binzhou Medical University Hospital, Binzhou 256600, China.
Objectives: The mechanism of the odontogenic differentiation of apical papillary cells (APCs) stimulated by bioactive glass 45S5 is still unclear. This study aims to investigate the effect of autophagy on the odontogenic differentiation of APCs stimulated by bioactive glass 45S5.
Methods: APCs were isolated and cultured , and the cell origin was identified by flow cytometry.
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