Article
Therapeutic reactivation of mutant p53 protein by quinazoline derivatives.
Investigational new drugs - 1 Oct 2012
Sutherland Hamish S, Hwang In Young, Marshall Elaine S, Lindsay Brent S, Denny William A, Gilchrist Catherine, Joseph Wayne R, Greenhalgh Debra, Richardson Emma, Kestell Philip, Ding Angela, Baguley Bruce C
Abstract excerpt
PURPOSE: The human tumour suppressor protein p53 is mutated in nearly half of human tumours and most mutant proteins have single amino acid changes. Several drugs including the quinazoline derivative 1 (CP-31398) have been reported to restore p53 activity in mutant cells. The side chain of 1 contains a styryl linkage that compromises its stability and we wished to explore the activity of analogues containing more...
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