Abstract

Objective: The objective of the study was to synthesize and evaluate the anticancer activity of some novel acridine derivatives.
 Methods: The present works involve condensation of acridine and various 2, 4-Thiazolidine-2,4-dione derivatives (2a–2h) with chloroacetyl chloride to give a novel acridine derivatives (5a–5l), respectively.
 Results: All the newly synthesized molecules (5a–5l) were characterized by FTIR, H1-NMR, and mass spectral analysis along with physical data. The biological potentials of the new synthesized compounds are evaluated for their in vitro anticancer activity by MTT assay.
 Conclusion: The synthesized compounds 5a, 5f, and 5h exhibited good anticancer activity against MCF-7 and SKVO3 cancer cell lines at a concentration of 0.5 mg/mL-1.

Highlights

  • Acridine was first isolated by Carl Grabe and Heinrich Caro in Germany in 1870 from high boiling fraction of coal tar [1]

  • Bernthsen reported the primary synthesis of acridine, in which diphenylamine was reacted with benzoic acid using zinc chloride and high temperatures

  • The present work involves the reaction between condensation of acridine and various 2, 4-Thiazolidine-2,4-dione derivatives (2a–2h) with chloroacetyl chloride to give a novel acridine derivatives (5a–5l), respectively

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Summary

Introduction

Acridine was first isolated by Carl Grabe and Heinrich Caro in Germany in 1870 from high boiling fraction of coal tar [1]. Bernthsen reported the primary synthesis of acridine, in which diphenylamine was reacted with benzoic acid using zinc chloride and high temperatures. The synthesis of acridine and its derivatives has attracted considerable attention from untreated and medicinal chemists for many natural life, as a number of natural source have been report to have this heterocyclic nucleus. Acridine is known by the names of dibenzopyridine, 2,3,5,6-dibenzopyridine, and 10-azaanthracene. It has an irritating odor and crystallizes in colorless to light yellow needles with melting point of 110°C and boiling point of 346°C

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