MUMBAI, India, Oct. 5 -- Intellectual Property India has published a patent application (202541029802 A) filed by Sumathy A; Nazrin Fathima A; N. L. Gowrishankar; Shamna Z; Manu M G; and Greeshma S on March 28, 2025, for Synthesis Of Chalcone Based Pyrimidines As Her2 Inhibitors Against Breast Cancer And Its Antioxidant Activity.
Inventors include Sumathy A; Nazrin Fathima A; N. L. Gowrishankar; Shamna Z; Manu M G; and Greeshma S.
The application for the patent was published on October 02, 2026, under issue no. 40/2026.
Abstract: Background and Objective: HER2 overexpressed Breast cancer is ubiquitous invasive type of cancer having global attention due to its high incidence rate. The resistance to current chemotherapies and cytotoxic effects necessitates the synthesis of newer agents. This current research work aim to design, insilico screening and synthesis of chalcone substituted heterocycles (pyrimidinones) against HER2 targeting breast cancer. Methods: Chalcone derived heterocycles mainly pyrimidinones were designed and screened computationally by different methods. The pharmacokinetic, physicochemical and drug likeness properties were analyzed using SWISS- ADME and toxicity determined by OSIRIS property explorer. The proposed derivatives were docked against HER2 (3PP0) by using Autodock vina integrated PyRx software and the binding affinities are determined. Selected compounds’ activity prediction was done. The synthesis was carried out by both microwave and conventional methods. The microwave assisted condensation of 4-dimethylamino benzaldehyde and substituted aromatic aldehydes results in the formation of chalcone. The cyclization of these substituted chalcone in presence of strong base and nucleophilic agents (urea) forms 4-[4-(dimethylamino)phenyl]-6-phenylpyrimidin-2(1H)- one derivatives. Pyrimidinone derivatives (PR1, PR2, PR3, and PR4) were elucidated by 13C NMR, 1H NMR and MASS spectroscopic methods. The anti-breast cancer activity was assessed on MCF7 cell line by MTT assay method. The radical scavenging activity also determined using DPPH method. Result: All the designed compounds have greater binding affinity at the active site of HER2 and have promising pharmacokinetic, druglikeness, physicochemical and toxicity property. The synthesized pyrimidinone derivatives have eminent anticancer activity in MCF7 cell line. PR3 and PR4 are the most potent among the four pyrimidinone derivatives. The compounds show radical scavenging scavenging activity also. Conclusion: On the basis of results, it can be concluded that the synthesized compounds have remarkable antibreast cancer potential against HER2 and have antioxidant activity. Keywords: Chalcone; Breast cancer; HER2; Pyrimidinones; MCF7
Disclaimer: Curated by HT Syndication.
