What is it about?

This research focuses on synthesizing and understanding the bioactivities of new benzene-imidazole fused-ring molecules and a series of benzimidazole derivatives. The molecules of interest portray potential inhibition properties for both PARP-1 and DHODH enzymes, which could benefit new anti-cancer agents designing. It could also serve as a contributor to drug designing and development by providing a platform for the construction of organic molecules. The synthesis of new molecules utilizing organic reactions could provide a theoretical basis to elaborate biological experimentation. This research mainly targets those cancer patients with BRCA-2 deficiency. Support from cancer society, physicians, funding from ministry and clinicians are needed for the progress of this research.

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Why is it important?

Chemotherapy treatment kills both cancerous and healthy cells, and it works throughout the whole body. There is a need for a better alternative with lesser side effects for cancer patients. Therefore, discovery and development of potent, selective and safe drugs are crucial. Benzimidazole derivatives possess good pharmacological and antitumor activity, including PARP and DHODH inhibition. Understanding the mechanisms of PARP-1 and DHODH enzymes in DNA replication and repair mechanisms involved in the hyper-proliferation of cancer cells and targeting the activity of these enzymes for anti-cancer therapy would be beneficial.


Cancer is a leading cause of death worldwide, and breast cancer accounts for 2.09 million cases. Treatment option for breast cancer usually comprises of surgery, chemotherapy and radiation therapy. Computational chemistry plays a role in drug design and discovery by identifying drug binding to its target and the chemical properties for designing potential new drugs. This machine learning method can accelerate the identification and design of potential new drugs for cancer treatment. This research provides a better insight into new drug development, and it aims to ensure healthy lives and promote well-being for all at all ages, which is in line with the UN’s third Sustainable Development Goal. Further research is needed to address the development and implication of machine learning towards effective cancer treatment.

Iskandar Abdullah
University of Malaya

Read the Original

This page is a summary of: Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH, Bioorganic & Medicinal Chemistry, August 2015, Elsevier, DOI: 10.1016/j.bmc.2015.05.051.
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