2-Deaminoactinomycin D, synthesis and interaction with deoxyribonucleic acid
- 1 August 1977
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 20 (8), 1055-1059
- https://doi.org/10.1021/jm00218a013
Abstract
2-Deaminoactinomycin D was synthesized and characterized. It binds to DNA by intercalation according to NMR, CD [circular dichroism], thermal denaturation and unwinding studies on the drug.sbd.DNA complex. Loss of the 2-amino group does not seriously affect binding parameters relative to actinomycin D. Affinity for calf thymus DNA may even be increased, according to .DELTA.Tm [melting temperature] measurements. The unwinding of circular DNA caused by this compound is at least as large as that affected by actinomycin D and ethidium bromide. 2-Deaminoactinomycin D is less effective than actinomycin D in inhibiting nucleic acid syntheses in L1210 mouse leukemia cell culture and in in vivo antitumor activity against P388 leukemia.This publication has 5 references indexed in Scilit:
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