Abstract

The radical Kolbe electrolysis can be applied to synthesize non-proteinogenic amino acids starting from ʟ-glutamic acid (or L-aspartic acid, respectively). Using suitable protecting groups for both amino and carboxy functionalities, the retention of chirality at the α-carbon atom can be expected.

Highlights

  • Quinacrine (IUPAC name: 4-N-(6-chloro-2-methoxyacridin-9-yl)-1-N,1-N-diethylpentane-1,4-diamine) is a synthetic drug belonging to the family of acridine-based synthetic compounds and the 9-aminoacridine subfamily

  • A few studies have presented evidence suggesting that quinacrine inhibits ribosome biogenesis (RBG) by suppressing the activity of the RPA194 catalytic subunit of RNA polymerase-I and nucleolar RBG nucleostemin (NS/GNL3), inducing nucleolar stress, which leads to a reduction in RAD51 recruitment to the DNA damage site and eventually causes disruption of the homologous recombination repair mechanism [49,51]

  • QC has been reported to promote the degradation of phosphorylated checkpoint kinase 1 (p-Chk1) and downregulate replication protein A (RPA), impairing base excision repair (BER) machinery

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Summary

Introduction

Quinacrine (IUPAC name: 4-N-(6-chloro-2-methoxyacridin-9-yl)-1-N,1-N-diethylpentane-1,4-diamine) is a synthetic drug belonging to the family of acridine-based synthetic compounds and the 9-aminoacridine subfamily. Low concentrations of QC have been shown to induce redistribution of Ca2+ ions, leading to disruption of IP3 dependent Ca2+ oscillation, hampering the growth of Plasmodium falciparum, as they exhibit stage-specific Ca2+oscillations in the ring form during the trophozoite stage, which is a key requirement for the maturation of the parasite inside erythrocytes. Owing to its fluorescent and DNA-binding properties, QC is routinely used in laboratories to stain chromosomes and study their patterns. This technique is explicitly called “Q-banding” [9,10,11]. QC was extensively utilized as a sterilizing agent in the 1980s [12,13]

Internalization and Pharmacokinetics of QC
Quinacrine and Cancer
Quinacrine and DNA Intercalation
Quinacrine Mediated Induction of P53 Signaling and Inhibition of NF-κB
Quinacrine and Inhibition of DNA Replication Enzymes
Quinacrine Induced Autophagy and Cell Cycle Arrest
Quinacrine and TRAIL Sensitivity
Quinacrine and Chemoresistance
Quinacrine Nanoparticles in Cancer Treatment
Clinical Research Studies of Quinacrine in Cancer Treatment
Findings
Conclusions
Full Text
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