N-Propargylated Isatin-Mannich Mono- and Bis-adducts: Synthesis and Preliminary Analysis of in Vitro Activity Against Tritrichomonas Foetus

Overview

Journal Eur J Med Chem

Specialty Chemistry

Date 2014 Feb 25

PMID 24561663

Citations 9

Authors

Nisha

Kewal Kumar

Gaurav Bhargava

Kirkwood M Land

Kai-Hsiang Chang

Reena Arora

Somdutta Sen

Vipan Kumar

Affiliations

Soon will be listed here.

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.

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