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pubmed-article:10866398pubmed:abstractTextThe design, synthesis, in vitro and in vivo activities of novel alpha-bromoacrylic derivatives of distamycin A, modified at the amidino moiety by the replacement with basic or non-basic groups are reported. In spite of the relevance of these modifications of distamycin frame, the new derivatives are potent cytotoxics. The presence of the amidino moiety, is, therefore; not an absolute requirement for the activity. In particular due to a favorable myelotoxicity/cytotoxicity ratio, guanidino derivative PNU 166196 was selected for clinical development.lld:pubmed
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pubmed-article:10866398pubmed:dateRevised2004-11-17lld:pubmed
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pubmed-article:10866398pubmed:articleTitleCytotoxic alpha-bromoacrylic derivatives of distamycin analogues modified at the amidino moiety.lld:pubmed
pubmed-article:10866398pubmed:affiliationDepartment of Chemistry, Pharmacia & Upjohn, Discovery Research Oncology, Milan, Italy. paolo.cozzi@eu.pnu.comlld:pubmed
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