On December 31, 2021, Damghani, Tahereh; Moosavi, Fatemeh; Khoshneviszadeh, Mehdi; Mortazavi, Motahareh; Pirhadi, Somayeh; Kayani, Zahra; Saso, Luciano; Edraki, Najmeh; Firuzi, Omidreza published an article.Related Products of 574-98-1 The title of the article was Imidazopyridine hydrazone derivatives exert antiproliferative effect on lung and pancreatic cancer cells and potentially inhibit receptor tyrosine kinases including c-Met. And the article contained the following:
Abstract: Aberrant activation of c-Met signalling plays a prominent role in cancer development and progression. A series of 12 imidazo [1,2-α] pyridine derivatives bearing 1,2,3-triazole moiety were designed, synthesized and evaluated for c-Met inhibitory potential and anticancer effect. The inhibitory activity of all synthesized compounds against c-Met kinase was evaluated by a homogeneous time-resolved fluorescence (HTRF) assay at the concentration range of 5-25 μM. Derivatives 6d, 6e and 6f bearing Me, tert-Bu and dichloro-Ph moieties on the triazole ring, resp., were the compounds with the highest potential. They significantly inhibited c-Met by 55.3, 53.0 and 51.3%, resp., at the concentration of 25 μM. Synthetic compounds showed antiproliferative effects against lung (EBC-1) and pancreatic cancer cells (AsPc-1, Suit-2 and Mia-PaCa-2) expressing different levels of c-Met, with IC50 values as low as 3.0 μM measured by sulforhodamine B assay. Active derivatives significantly blocked c-Met phosphorylation, inhibited cell growth in three-dimensional spheroid cultures and also induced apoptosis as revealed by Annexin V/propidium iodide flow cytometric assay in AsPc-1 cells. They also inhibited PDGFRA and FLT3 at 25 μM among a panel of 16 kinases. Mol. docking and dynamics simulation studies corroborated the exptl. findings and revealed possible binding modes of the select derivatives with target receptor tyrosine kinases. The results of this study show that some imidazopyridine derivatives bearing 1,2,3-triazole moiety could be promising molecularly targeted anticancer agents against lung and pancreatic cancers. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Related Products of 574-98-1
The Article related to antiproliferative effect lung pancreatic cancer cell tyrosine kinase, Placeholder for records without volume info and other aspects.Related Products of 574-98-1
Referemce:
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