Hybrid compounds as new Bcr/Abl inhibitors.

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Wang D, Zhang Z, Lu X, Feng Y, Luo K, Gan J, Yingxue L, Wan J, Li X, Zhang F, Tu Z, Cai Q, Ren X, Ding K

Hybrid compounds as new Bcr/Abl inhibitors.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):1965-8. doi: 10.1016/j.bmcl.2011.02.029. Epub 2011 Feb 13.

PubMed ID

21376587 [ View in PubMed

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Abstract

A series of 2,4-disubstituted thiazole derivatives were designed and synthesized as new Bcr/Abl inhibitors by hybriding the structural moieties from FDA approved imatinib, nilotinib and dasatinib. The new inhibitors strongly suppressed the activity of Bcr/Abl kinase and potently inhibited the proliferation of K562 and KU812 leukemia cancer cells. Compound 4i displayed comparable potency with that of nilotinib in both biochemical kinase assay and cancer cell growth inhibition assay. These inhibitors might serve as lead compounds for further developing new anticancer drugs.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Imatinib	Tyrosine-protein kinase ABL1	IC 50 (nM)	309	N/A	N/A	Details
Nilotinib	Tyrosine-protein kinase ABL1	IC 50 (nM)	39.3	N/A	N/A	Details