14 research outputs found

    Synthesis of some new oxazolinyl/thia-zolinyl/imidazolinyl- benzoxazoles, benzothiazoles and benzimidazoles

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    942-948A new class of oxazolinyl/thiazolinyl/imidazolinyl-benzo­xazoles/benzothiazoles/benzimidazoles have been prepared by exploiting the respective heterocyclic sulfonyl acetic acid methyl ester functionality with different nucleophiles using samarium(III) chloride

    Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole

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    A variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio, methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic activities. The compound pyrimidinyl bis methylthio benzimidazole 22 was a potent antimicrobial agent particularly against Staphylococcus aureus (29 mm, MIC 12.5 mu g/mL) and Penicillium chrysogenum (38 mm, MIC 12.5 mu g/mL). The amino linked pyrimidinyl bis benzothiazole 24 exhibited cytotoxic activity on A549 cells with IC50 value of 10.5 mu M. (C) 2014 Elsevier Masson SAS. All rights reserved

    Chemical synthesis of histone H2A with methylation at Gln104

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    Histone H2A methylation at Gln104 (H2AQ104Me) is a new type of histone post-translational modification (PTM) discovered recently. This modification has been found to have significant influence on gene transcription. However, the structural and functional consequence of glutamine methylation on nucleosome remains to be further elucidated. Obtaining of histones with site-specific methylation at glutamine residues might facilitate the studies towards a better understanding of this new PTM. In the present work, total chemical synthesis of H2AQ104Me was carried out through use of the hydrazide-based native chemical ligation. Synthetic histone H2AQ104Me could be successfully incorporated into nucleosomes in vitro and showed a negative influence on the nucleosome stability.National Basic Research Program of China [2013CB932800]; National Natural Science Foundation of China [21532004, 21225207, 81621002]SCI(E)ARTICLE5621-6276
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