Synthesis and Biological Evaluation of Novel 1H-Benzo[d]imidazole Derivatives as Potential Anticancer Agents Targeting Human Topoisomerase I was written by Pandey, Stuti;Tripathi, Pragya;Parashar, Palak;Maurya, Vikas;Malik, Zubbair Md.;Singh, Raja;Yadav, Pooja;Tandon, Vibha. And the article was included in ACS Omega in 2022.Reference of 21867-64-1 This article mentions the following:
Small mols. that modulate biol. functions are targets of modern-day drug discovery efforts. A new series of novel 1H-benzo[d]imidazoles (BBZs) were designed and synthesized with different functional groups at the Ph ring and variable lengths of the alkyl chain at the piperazine end as anticancer agents. We identified human topoisomerase I (Hu Topo I) as a probable target of these mols. through a computational study and DNA relaxation assay, a functional assay of the Hu Topo I enzyme. UV absorption, fluorescence, and CD spectroscopy were used to study interactions between BBZ and DNA. Out of 16 compounds, three substances showed strong binding affinity and thermal stabilization of AT sequence-specific DNA. BBZs were screened against a panel of 60 human cancer cell lines at National Cancer Institute, USA. Most potent mols. showed 50% growth inhibition (GI50) in a concentration range from 0.16 to 3.6μM cancer cells. Moreover, one compound showed 50% inhibition of the relaxation of DNA by Hu Topo I at 16μM. Furthermore, flow cytometry revealed that the three substances cause prominent G2M arrest of cancer cells. In view of the above, we propose that I deserves to be further evaluated for its therapeutic use as an anticancer agent. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Reference of 21867-64-1).
1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Reference of 21867-64-1
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics