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Tricyclic thiazoles are a new class of angiogenesis inhibitors.

ABSTRACT: Tricyclic thiazoleamine derivatives that were identified as hits in a screen against human umbilical vein endothelial cell proliferation were subjected to a structure-activity relationship study. Two structurally superimposable scaffolds-4H-thiochromeno[4,3-d]thiazol-2-amine and 5,6-dihydro-4H-benzo[6,7]cyclohepta[1,2-d]thiazol-2-amine derivatives-yielded low-micromolar inhibitors, and two among them 37 and 43 also exhibited antiangiogenic activity in an endothelial tube formation assay. Thus, 37 and 43 can serve as leads to develop a novel class of antiangiogenic agents.

SUBMITTER: Bhat S

PROVIDER: S-EPMC3670749 | biostudies-literature | 2013 May

REPOSITORIES: biostudies-literature

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Tricyclic thiazoles are a new class of angiogenesis inhibitors.

Bhat Shridhar S Shim Joong Sup JS Liu Jun O JO

Bioorganic & medicinal chemistry letters 20130224 9

Tricyclic thiazoleamine derivatives that were identified as hits in a screen against human umbilical vein endothelial cell proliferation were subjected to a structure-activity relationship study. Two structurally superimposable scaffolds-4H-thiochromeno[4,3-d]thiazol-2-amine and 5,6-dihydro-4H-benzo[6,7]cyclohepta[1,2-d]thiazol-2-amine derivatives-yielded low-micromolar inhibitors, and two among them 37 and 43 also exhibited antiangiogenic activity in an endothelial tube formation assay. Thus, 3 ...[more]

PMID: 23518276

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