Discovery of novel JAK2 and EGFR inhibitors from a series of thiazole-based chalcone derivatives

Kamonpan Sanachai, Thitinan Aiebchun, Panupong Mahalapbutr, Supaphorn Seetaha, Lueacha Tabtimmai, Phornphimon Maitarad, Iakovos Xenikakis, Athina Geronikaki, Kiattawee Choowongkomon, Thanyada Rungrotmongkol

RSC Medicinal Chemistry · 2021 · 45 citations · 68 references

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Abstract

formed a hydrogen bond with Met769 at the hinge region, Lys721 near a glycine loop, and Asp831 at the activation loop of EGFR. Altogether, these potent thiazole derivatives, following Lipinski's rule of five, could likely be developed as a promising JAK2/EGFR targeted drug(s) for cancer therapy.

References

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