Total Synthesis of Bleomycin A2 and Related Agents. 1. Synthesis and DNA Binding Properties of the Extended C-Terminus: Tripeptide S, Tetrapeptide S, …

…, SL Colletti, T Honda, RF Menezes

Index: Boger, Dale L.; Colletti, Steven L.; Honda, Takeshi; Menezes, Royce F. Journal of the American Chemical Society, 1994 , vol. 116, # 13 p. 5607 - 5618

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Citation Number: 89

Abstract

Abstract: Full details of concise, diastereocontrolled syntheses of 2-5 and their incorporation into tri-, tetra-, and pentapeptide S, the C-terminus of bleomycin A2, are described. The extension of the studies to the synthesis of a complete set of tri-and tetrapeptide S structural analogs 29a, b and 43b-j is detailed, and their DNA binding constants (apparent KB, calf thymus DNA) and apparent binding site sizes were determined. Consistent with past ...