Synthesis and Biological Evaluation of Novel Phenothiazine Derivatives as Potential Antitumor Agents

Abstract

Phenothiazines ˗ Antipsychotic drugs, which have been studied from centuries and attracted researcher’s attention toward its antitumor activities apart from their fundamental neuroleptic properties. Hence, we have targeted different structures of phenothiazines to develop potent antitumor agents. In the present study, we have synthesized various heterocyclic derivatives incorporating phenothiazine compounds via one-pot multicomponent reaction by means of N-alkyl-3-formylphenothiazine under reflux/ultrasonic method and different spectral characterization techniques such as FT-IR, mass, ¹H and ¹³C NMR spectroscopy were used to validate the molecular structures of the synthesized compounds. The antitumor properties of all the synthesized compounds were investigated using MTT and LDH assay against HeLa cell lines. The results shown that the compounds 4 b, 2a and 3a have maximum LDH release (57.69 ± 4.69, 57.7 ± 4.6 & 67.8 ± 4.9) at 1000 µg concentration.

Keywords:

• Phenothiazines
• antitumor agents
• HeLa cells
• MTT assay
• LDH assay

Acknowledgments

The authors gratefully acknowledge the management of VIT University, Vellore and CVR College of Engineering for encouraging and providing the necessary facilities for carrying out this work. Also, authors acknowledge SAIF IIT Madras and SIF VIT University for recording the spectral data.

Disclosure statement

No potential conflict of interest was reported by the authors.