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Novel pyrimido-pyridazine derivatives: design, synthesis, anticancer evaluation and in silico studies

Publication Type : Journal Article

Publisher : Future Medicinal Chemistry

Url : https://doi.org/10.4155/fmc-2022-0199

Campus : Kochi

School : School of Pharmacy

Year : 2022

Abstract : Aim: A novel pyrimido-pyridazine derivative for developing anticancer agents was synthesized via Ullmann arylation using an efficient Cu(OAc)2 catalyst. Materials & methods: Compounds were investigated for their anticancer potential, against human breast adenocarcinoma cells, viz. MCF-7, MDA-MB-231 and normal cell line HEK-293. Further, an in vivo study was conducted on lymphoma-bearing mice while in silico analysis was carried out for molecular interactions.
Results: Compound 2b displayed significant antitumor activity towards MDA-MB-231 cells through induction of apoptosis and arresting cells in S-phase in vitro, while it significantly increased the lifespan and reduced tumor growth in vivo. An in silico study revealed potent tyrosine-protein kinase inhibitors. Conclusion: Taken together the molecule has the potential to become an effective therapeutic treatment for breast cancer.

Cite this Research Publication : Priyanka Sonker, Mamata Singh, Manisha Nidhar, Vishal Prasad Sharma, Priyanka Yadav, Rashmi Singh, Biplob Koch, and Ashish Kumar Tewari, Novel pyrimido-pyridazine derivatives: design, synthesis, anticancer evaluation and in silico studies, Future Medicinal Chemistry, 2022, https://doi.org/10.4155/fmc-2022-0199.

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