What is it about?
Novel pyrimidine derivatives were designed, synthesized, and evaluated against breast cancer cell lines. Compound R8 significantly inhibited the growth of breast cancer cells such as MDA-MB-231 and MCF-7. The Molecular docking studies also revealed and support that compound R8 has good fitting by forming different Hydrogen bonding interactions with amino acids at the ATP binding site of epidermal growth factor receptor (EGFR). Compound R8 was a promising lead molecule that showed better results as compared to other compounds in in-vitro studies.
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Why is it important?
Our research work shows that pyrimidine derivatives act as EGFR/HER2 inhibitors for barest cancer. We screened the synthesized compounds based on their cytotoxicity activity by employing MTT assay and further enzyme inhibition assay. Molecular docking studies supports and proved that compound R8 has good binding affinity and it fits into ATP binding sites of EGFR receptor.
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This page is a summary of: Design, Synthesis, In Silico and In Vitro Evaluation of Novel Pyrimidine Derivatives as EGFR Inhibitors, Anti-Cancer Agents in Medicinal Chemistry, July 2020, Bentham Science Publishers, DOI: 10.2174/1871520620666200721102726.
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