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Researchers synthesise novel compounds with DNA binding and anticancer potential

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Scientists are always on the lookout for novel chemical compounds with medicinal properties to fight many of the diseases we know. In one such effort, researchers from the Aligarh Muslim University, Uttar Pradesh, and their collaborators have developed three compounds with steroids and pyrimidines with remarkable biological applications. The results of the study are published in the International Journal of Biological Macromolecules.

The novel chemicals compounds, called ‘steroidal pyrimidines’, were synthesised in a laboratory by combining the compound steroidal thiosemicarbazone, with another compound called (2-methyl) diethyl malonate. The researchers then explored how these compounds interact with the DNA molecule in our cell and also studied the anticancer potential of these compounds.

The study showed that all the three steroidal pyrimidines had a strong affinity for the DNA molecule. To get an insight into the interaction process, the researchers used molecular docking—a computer-based approach to predict the orientation of a molecule in a compound. Docking indicated that in spite of their large size, the steroidal pyrimidines interact with the minor groove—a shallow furrow in the DNA molecule.

Interestingly, one of the newly synthesised compounds has a unique ability to cleave into the DNA molecule—a task that is not easy considering the stability of the phosphodiester bonds linking the nucleotides in a DNA molecule. DNA cleaving agents are vital in molecular biology for uses like insertion of a human gene in a bacterial DNA or preparation of recombinant DNA. Although some metal compounds can cleave the DNA, they are not preferred because of their toxicity.

When the researchers experimented the use of the steroidal pyrimidines with human cancer cells, they observed that the compounds have anticancer potential and one of these compounds was able to kill the cancer cells by inducing apoptosis—a tightly controlled cell suicide process. This compound, the researchers predict, has an excellent prospect to act as a cancer chemotherapeutic candidate in the future.

“The present study has shown that these synthesised steroidal pyrimidines can be used as a template for future modifications to design more potent and selective cell killing and DNA binding agents”, remark the authors on the potential applications of the compounds.