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Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1

✍ Scribed by Carine Aubry; A. James Wilson; Daniel Emmerson; Emma Murphy; Yu Yam Chan; Michael P. Dickens; Marcos D. García; Paul R. Jenkins; Sachin Mahale; Bhabatosh Chaudhuri


Book ID
108072679
Publisher
Elsevier Science
Year
2009
Tongue
English
Weight
608 KB
Volume
17
Category
Article
ISSN
0968-0896

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The synthesis of new analogues of Arcyriaflavin A in which one indole ring is replaced by an aryl or heteroaryl ring is described. These new series of aryl[a]pyrrolo[3,4-c]carbazoles were evaluated as inhibitors of Cyclin D1-CDK4. A potent and selective D1-CDK4 inhibitor, 7a (D1-CDK4 IC 50 =45 nM),