Synthesis of new cytotoxic E-ring modified camptothecins

S Cananzi, S Dallavalle, A Bargiotti, L Merlini, R Artali…

Index: Cananzi, Salvatore; Dallavalle, Sabrina; Bargiotti, Alberto; Merlini, Lucio; Artali, Roberto; Beretta, Giovanni Luca Tetrahedron Letters, 2010 , vol. 51, # 50 p. 6489 - 6492

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Abstract

One of the major limitations of CPT and analogues is the severe toxicity, stemming in part from the instability of the α-hydroxylactone E-ring. This ring plays a key role in supporting both efficient Topo I inhibition and in vivo potency. Three-dimensional structure analyses of a ternary complex formed between TopoI, DNA and Topotecan by X-ray crystallography showed that the drug interacts both with the DNA base pairs flanking the cleavage sites and three key aminoacid ...

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