N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus

作者：Nisha; Kumar Kewal; Bhargava Gaurav; Land Kirkwood M; Chang Kai Hsiang; Arora Reena; Sen Somdutta; Kumar Vipan^*

来源：European Journal of Medicinal Chemistry, 2014, 74: 657-663.

DOI：10.1016/j.ejmech.2014.01.015

• N-Propargylated-isatin Mannich adducts
• N-Propargylated-isatin-7-chloroquinoline
• conjugates
• Tritrichomonas foetus
• Cytotoxicity

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.

• 出版日期2014-3-3