Truncated azinomycin analogues intercalate into DNA.
Casely-Hayford, M.A. ; ; Patterson, Laurence H. ; Gerner, C. ; Neidle, S. ; Searcey, M.
Casely-Hayford, M.A.
Patterson, Laurence H.
Gerner, C.
Neidle, S.
Searcey, M.
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2005
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Abstract
The design and synthesis of a potentially more therapeutically-viable azinomycin analogue 4 based upon 3 has been completed. It involved coupling of a piperidine mustard to the acid chloride of the azinomycin chromophore. Both the designed azinomycin analogue 4 and the natural product 3 bind to DNA and cause unwinding, supporting an intercalative mode of binding.
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A designed analogue of the left half of azinomycin has been synthesized and unwinds supercoiled DNA.
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Casely-Hayward, M., Pors, K., Patterson, L.H. and Gerner, C. et al. (2005). Truncated azinomycin analogues intercalate into DNA. Bioorganic Medicinal Chemistry Letters. Vol. 15, No. 3, pp. 653-656.
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