Potentiation of PBD Dimers by Lipophilicity Manipulation
نویسندگان
چکیده
منابع مشابه
Antistaphylococcal activity of DNA-interactive pyrrolobenzodiazepine (PBD) dimers and PBD-biaryl conjugates
OBJECTIVES Pyrrolobenzodiazepine (PBD) dimers, tethered through inert propyldioxy or pentyldioxy linkers, possess potent bactericidal activity against a range of Gram-positive bacteria by virtue of their capacity to cross-link duplex DNA in sequence-selective fashion. Here we attempt to improve the antibacterial activity and cytotoxicity profile of PBD-containing conjugates by extension of dime...
متن کاملEffect of base sequence on the DNA cross-linking properties of pyrrolobenzodiazepine (PBD) dimers
Pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimers are synthetic sequence-selective DNA minor-groove cross-linking agents that possess two electrophilic imine moieties (or their equivalent) capable of forming covalent aminal linkages with guanine C2-NH(2) functionalities. The PBD dimer SJG-136, which has a C8-O-(CH(2))(3)-O-C8'' central linker joining the two PBD moieties, is currently undergoing p...
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In this study, the existence of biological potential of selected N-(substituted phenyl)-2-chloroacetamides was examined none empirically, as was the possibility of applying simpleexperimental technique in predicting essential properties which affect the biological activityof the compounds. By applying the Lipinski and Ghose’s rules, it has been revealed that theexamined chloroacetamides fulfill...
متن کاملPrediction of Lipophilicity and Pharmacokinetics of Chloroacetamides by Chemometric Approach
In this study, the existence of biological potential of selected N-(substituted phenyl)-2-chloroacetamides was examined none empirically, as was the possibility of applying simpleexperimental technique in predicting essential properties which affect the biological activityof the compounds. By applying the Lipinski and Ghose’s rules, it has been revealed that theexamined chloroacetamides fulfill...
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ژورنال
عنوان ژورنال: Current Topics in Medicinal Chemistry
سال: 2019
ISSN: 1568-0266
DOI: 10.2174/1568026619666190401112517