Chemical structure of phenothiazines and their biological activity

A Jaszczyszyn, K Gąsiorowski, P Świątek… - Pharmacological …, 2012 - Springer
A Jaszczyszyn, K Gąsiorowski, P Świątek, W Malinka, K Cieślik-Boczula, J Petrus…
Pharmacological Reports, 2012Springer
Phenothiazines belong to the oldest, synthetic antipsychotic drugs, which do not have their
precursor in the world of natural compounds. Apart from their fundamental neuroleptic action
connected with the dopaminergic receptors blockade, phenothiazine derivatives also exert
diverse biological activities, which account for their cancer chemopreventive-effect, as:
calmodulin-and protein kinase C inhibitory-actions, anti-proliferative effect, inhibition of P-
glycoprotein transport function and reversion of multidrug resistance. According to literature …
Abstract
Phenothiazines belong to the oldest, synthetic antipsychotic drugs, which do not have their precursor in the world of natural compounds. Apart from their fundamental neuroleptic action connected with the dopaminergic receptors blockade, phenothiazine derivatives also exert diverse biological activities, which account for their cancer chemopreventive-effect, as: calmodulin-and protein kinase C inhibitory-actions, anti-proliferative effect, inhibition of P-glycoprotein transport function and reversion of multidrug resistance. According to literature data on relations between chemical structure of phenothiazines and their biological effects, the main directions for further chemical modifications have been established. They are provided and discussed in this review paper.
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