Macromolecular Conjugates of 4- and 8-Aminoquinoline Compounds |
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Authors: | B A Aderibigbe E W Neuse |
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Affiliation: | (1) School of Chemistry, University of Witwatersrand, Wits, 2050, South Africa |
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Abstract: | Some members of 4-aminoquinolines and 8-aminoquinolines have been found to provide adjuvant effects when used in combination
with anti-cancer drugs. The clinical co-administration of active anti-cancer drugs with other drugs acting as potentiating
agents has shown considerable merits when compared to a single-drug administration. Anti-cancer drugs are often toxic when
delivered straight, but the bio-reversible drug conjugation of anticancer drugs to water-soluble macromolecular carriers has
proved to enhance the therapeutic effectiveness of anticancer drugs. Following facilitated pharmacokinetics pathways, the
conjugates, acting as pro-drugs, will release the active drug species in the transformed target cells and their designs are
geared towards reducing pharmacological barriers of toxicity, drug resistance and poor bioavailability encountered with currently
used anti-cancer drugs. This paper describes the synthesis of water-soluble macromolecular carriers containing 4- and 8-aminoquinolines
that are bio-reversibly anchored with cytotoxic drugs. The conjugates and co-conjugates are isolated as water soluble solids
and characterized by NMR-spectroscopy. |
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