期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 74, 期 -, 页码 657-663出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.01.015
关键词
N-Propargylated-isatin Mannich adducts; N-Propargylated-isatin-7-chloroquinoline; conjugates; Tritrichomonas foetus; Cytotoxicity
资金
- University Grants Commission (UGC) under Rajiv Gandhi fellowship
- pacific Fund summer Undergraduate Research Fellowship at the University of Pacific
Cu(I)Cl promoted synthesis of N-propargylated-isatin Mannich mono- and bis-adducts with an extension towards the synthesis of N-propargylated-isatin-7-chloroquinoline conjugates was described. The synthesized scaffolds were evaluated for their in vitro activity against the veterinary protozoal pathogen Tritrichomonas foetus and cytotoxicity against human prostate (PC-3) cancer cell line. The preliminary evaluation data revealed the enhancement in the activity profiles with the introduction of 7-chloroquinoline ring with the most active conjugates 7a, 7c and 7d exhibiting an IC50 of 22.2, 11.3 and 24.5 mu M respectively against T. foetus and minimal toxicity against human prostate (PC-3) cell lines. (C) 2014 Elsevier Masson SAS. All rights reserved.
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