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. 2014 Mar 3:74:657-63.
doi: 10.1016/j.ejmech.2014.01.015. Epub 2014 Jan 18.

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

Nisha  1 , Kewal Kumar  1 , Gaurav Bhargava  2 , Kirkwood M Land  3 , Kai-Hsiang Chang  3 , Reena Arora  4 , Somdutta Sen  4 , Vipan Kumar  5
Affiliations

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

Nisha et al. Eur J Med Chem. .

Abstract

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 μM respectively against T. foetus and minimal toxicity against human prostate (PC-3) cell lines.

Keywords: Cytotoxicity; N-Propargylated-isatin Mannich adducts; N-Propargylated-isatin-7-chloroquinoline conjugates; Tritrichomonas foetus.

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Figures

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Graphical abstract
Scheme 1
Scheme 1
Cu(I)Cl promoted N-propargylated isatin Mannich adducts.
Scheme 2
Scheme 2
Cu(I)Cl promoted N-propargylated isatin-quinoline Mannich adducts.
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