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

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 IC?? of 22.2, 11.3 and 24.5 ?M respectively against T. foetus and minimal toxicity against human prostate (PC-3) cell lines.

SUBMITTER: Nisha

PROVIDER: S-EPMC7115568 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature

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

Nisha Kumar Kewal K Bhargava Gaurav G Land Kirkwood M KM Chang Kai-Hsiang KH Arora Reena R Sen Somdutta S Kumar Vipan V

European journal of medicinal chemistry 20140118

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- ...[more]

PMID: 24561663

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