Abstract
The piperazine ring system is among the medicinally important nitrogen-containing heterocyclic ring systems and is exploited for the synthesis of various drug molecules. A number of FDA-approved anticancer drugs contain piperazine rings and thus it is considered as an attractive scaffold having extraordinary potential for the development of new anticancer agents. In recent decades there has been an alarming increase in the number of people suffering from cancerous diseases all over the world, which resulted in an extraordinary increase in research reports on new anticancer drug candidates. The aim of this article is to highlight the structural parameters imparting anticancer activity to piperazine derivatives and to indicate future perspectives for the discovery of new anticancer agents.
Highlights
Cancer is an uncontrolled proliferation of cells and has become a public health concern all over the world
The anticancer activity of the dendrimers was evaluated and significant efficacy was observed for piperazine-terminated organo-iron dendrimers against HTB26 and MCF7 cancer cell lines with IC 50 values of 3.6 μM and 2.5 μM, respectively
Piperazinecontaining compound showed moderate activity against HOP-92, having a growth percentage (GP %) value of 35.41%, while compound was moderately active against HT29, having a growth percentage value of 57.89% using a single dose of 10 μM concentration. 92,93 Among a series of pyrazolopyrimidine derivatives, piperazine-containing compound displayed antitumor activity against breast and lung cancer cell lines, having IC 50 values of 0.70 μmol/mL and 0.88 μmol/mL, respectively
Summary
Cancer is an uncontrolled proliferation of cells and has become a public health concern all over the world. This article comprehensively deals with the recent research work on piperazine derivatives having anticancer activity and highlights the structural parameters responsible for their bioactivity. Piperazine-containing polymeric anticancer agents In 2016, organo-iron complexes containing 1,4-dipiperazinobenzene-cyclopentadienyliron hexafluorophosphate were synthesized and were evaluated against two breast cancer cell lines, HTB26 and MCF7. Compound 14 (Figure 2) exhibited prominent activity against the HTB26 and MCF7 cell lines, having IC 50 values of 14 μM for both. The anticancer activity of the dendrimers was evaluated and significant efficacy was observed for piperazine-terminated organo-iron dendrimers against HTB26 and MCF7 cancer cell lines with IC 50 values of 3.6 μM and 2.5 μM, respectively. Metal complexes of piperazine derivatives The metal-containing anticancer drugs cisplatin and carboplatin are effective in the treatment of testicular, ovarian, and colorectal cancer. Compounds 22 and 23 were found to be more toxic, having IC 50 values of 0.11 and 0.35 μM, respectively, compared to the standard drug cisplatin. 44
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