title: 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 IC₅₀ of 22.2, 11.3 and 24.5 μM respectively against T. foetus and minimal toxicity against human prostate (PC-3) cell lines.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
authors.lastname: Nisha
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
authors.forename: Kewal
authors.initials: K
authors.lastname: Kumar
authors.affiliation: Department of Applied Sciences, Punjab Technical University, Kapurthala 144601, India.
authors.forename: Gaurav
authors.initials: G
authors.lastname: Bhargava
authors.affiliation: Department of Biological Sciences, University of the Pacific, Stockton, CA 95211, USA.
authors.forename: Kirkwood M
authors.initials: KM
authors.lastname: Land
authors.affiliation: Department of Biological Sciences, University of the Pacific, Stockton, CA 95211, USA.
authors.forename: Kai-Hsiang
authors.initials: KH
authors.lastname: Chang
authors.affiliation: Pharmacology Department, Sphaera Pharma Pvt. Ltd, Manesar 12205, India.
authors.forename: Reena
authors.initials: R
authors.lastname: Arora
authors.affiliation: Pharmacology Department, Sphaera Pharma Pvt. Ltd, Manesar 12205, India.
authors.forename: Somdutta
authors.initials: S
authors.lastname: Sen
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: vipan_org@yahoo.com.
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D066298:In Vitro Techniques; D007510:Isatin / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D016835:Tritrichomonas foetus / Q000187:drug effects*
chemical_list: D000981:Antiprotozoal Agents; D007510:Isatin
keywords: Cytotoxicity; N-Propargylated-isatin Mannich adducts; N-Propargylated-isatin-7-chloroquinoline conjugates; Tritrichomonas foetus