Minor groove binders are one of the most widely studied class of agents characterized by a high level of sequence specificity and they are still an interesting class of DNA ligands which demonstrate to possess several biological activities. It is important to underlie that in order to be effective as an anticancer agent, a minor groove binder should covalently and irreversibly bind the DNA with a long permanence of DNA lesion. This presentation will focus on cytotoxics structurally related from main minor groove binders such as distamycin A (1) , anthramycin (2) and CC-1065 (3). In particular, it will be underline the synthesis and biological activity of molecular hybrids deriving among the combination of the distamycin A and naturally occurring alkylating agents. In the lecture will be presented also the synthesis and the exceptional biological potency of a sulphur analog of Duocarmycin SA and CC-1065.
DNA Minor Groove Binders: the sulphur analog of duocarmicycin SA and CC-1065
BARALDI, Pier Giovanni
2008
Abstract
Minor groove binders are one of the most widely studied class of agents characterized by a high level of sequence specificity and they are still an interesting class of DNA ligands which demonstrate to possess several biological activities. It is important to underlie that in order to be effective as an anticancer agent, a minor groove binder should covalently and irreversibly bind the DNA with a long permanence of DNA lesion. This presentation will focus on cytotoxics structurally related from main minor groove binders such as distamycin A (1) , anthramycin (2) and CC-1065 (3). In particular, it will be underline the synthesis and biological activity of molecular hybrids deriving among the combination of the distamycin A and naturally occurring alkylating agents. In the lecture will be presented also the synthesis and the exceptional biological potency of a sulphur analog of Duocarmycin SA and CC-1065.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
