Phenothiazines as anti-cancer agents: SAR overview and synthetic strategies

Eur J Med Chem. 2023 Jun 5:254:115337. doi: 10.1016/j.ejmech.2023.115337.

Arun Kumar ¹, Chiara Vigato ², Donatella Boschi ², Marco Lucio Lolli ³, Deepak Kumar ⁴

Affiliations

1 Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, 173 229, India.
2 Department of Science and Drug Technology, University of Torino, via Pietro Giuria 9, 10125, Torino, Italy.
3 Department of Science and Drug Technology, University of Torino, via Pietro Giuria 9, 10125, Torino, Italy. Electronic address: [email protected].
4 Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, 173 229, India. Electronic address: [email protected].

PMID: 37060756 DOI: 10.1016/j.ejmech.2023.115337

Abstract

Cancer is a leading cause of death worldwide and there are still limited options for cure. Chemotherapy is the most significant treatment for Cancer which increased survival rates, despite this, it is associated with numerous side effects, as well as Cancer relapsing due to drug resistance insurgence; consequently, it is still a challenging task to develop new potent and less toxic anti-cancer agents for patients' care. Phenothiazine moiety, which leads a class of well-known antipsychotic drugs, possesses a wide range of biological activities and has been also introduced in Cancer chemotherapy. This review aims in disclosing the use of phenothiazines during the last five years for the development of different anti-cancer drug candidates. The design and the synthetic strategies adopted, the SAR investigations and the role of reviewed phenothiazine derivatives as anti-cancer agents and multi-drug resistance (MDR) reversals are here fully described and discussed.

Keywords

Anti-Cancer; MDR reversal; Phenothiazine; SAR; Synthesis.

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