Abstract

Nitrogen heterocyclic compounds are used in the pharmaceutical industry, in medicine and in agriculture for their biological activity. 4-Amino-3-acetylquinoline, a new synthetically prepared quinoline derivative, was the most effective compound in our primary cytotoxic screening. In this study, we evaluated cytotoxic/antiproliferative activity of quinoline using murine leukemia cell line L1210. Its ability to induce apoptosis was studied, too. Quinoline derivative acted cytotoxically on tumor cell line L1210, the IC(100) value were 50 microg/ml (for 24 h), 25 microg/ml (for 48 h) and 10 microg/ml (for 72 h). The IC(50) values was found to be less than 4 microg/ml, a limit put forward by the National Cancer Institute (NCI) for classification of he compound as a potential anticancer drug. The cytotoxic concentrations of 4-amino-3-acetyl quinoline induced morphological changes of L1210 cells and the apoptotic DNA fragmentation.

Highlights

  • Nitrogen heterocyclic compounds are used in the pharmaceutical industry, in medicine and in agriculture for their biological activity

  • We used murine leukemia cell line L1210 which was grown in supplemented RPMI 1640 medium (Biocom Bratislava) at 37 ̊C in a humidified atmosphere containing 5% CO

  • Cell viability were assessed by 0.4% trypan blue staining. 4-Amino-3-acetylquinoline (AAQ) prepared by Černuchová et al.[9], was dissolved in dimethyl sulfoxide (DMSO)

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Summary

Introduction

Nitrogen heterocyclic compounds are used in the pharmaceutical industry, in medicine and in agriculture for their biological activity. They have been the subject of chemical and biological studies due to their antimicrobial, antipyretic, analgesic, anti-inflammatory, herbicidal, fungicidal, antiviral and leishmanicidal properties. As documented in the literature, many derivatives act as anticancer active compounds[1,2,3,4]. There are a number of DNA topoisomerase inhibitors in development These have broad spectrum of activity against different kinds of human cancers.

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