Tricyclic thiazoles are a new class of angiogenesis inhibitors.

Tricyclic thiazoles are a new class of angiogenesis inhibitors.
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DOI:
10.1016/j.bmcl.2013.02.067
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发表时间:
2013-05-01
影响因子:
2.7
通讯作者:
Liu, Jun O.
Liu, Jun O.
中科院分区:
医学4区
文献类型:
--
作者:
Bhat, Shridhar;Shim, Joong Sup;Liu, Jun O.

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Tricyclic thiazoleamine derivatives that were identified as hits in a screen against human umbilica 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.
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