Man-designed bleomycins. synthesis of dioxygen activating molecules and a DNA cleaving molecule based on bleomycin-Fe(II)-02 complex |
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| Affiliation: | 1. Ashok & Rita Patel Institute of Integrated Study & Research in Biotechnology and Allied Sciences (ARIBAS), Sardar Patel University, New V. V. Nagar 388121, Gujarat, India;2. Department of Advanced Organic Chemistry, P. D. Patel Institute of Applied Sciences (PDPIAS), Charotar University of Science & Technology (CHARUSAT), Changa 388421, Gujarat, India;3. Navgujarat Science College, Balasinor, Mahisagar 388255, Gujarat, India;1. Department of Organic Chemistry and Centro de Innovación en Química Avanzada (ORFEO-CINQA), Faculty of Sciences, University of Alicante, E-03080 Alicante, Spain;2. Instituto de Síntesis Orgánica, Faculty of Sciences, University of Alicante, Spain |
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| Abstract: | A synthetic model for the metal binding site of bleomycin with a 4-methoxypyridine nucleus and atert-butyl group is shown to be comparable to bleomycin in terms of dioxygen activation. This model ligand is coupled with a DNA affinity moiety, tetrapeptide S, to afford a mandesigned bleomycin which exhibits potent DNA cleaving activityin vitro. |
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