Abstract
AbstractTo synthesize targeting polymeric antitumor agents, poly[(2‐acetoxy‐3,4‐dihydro‐2H‐pyran)‐alt‐(maleic anhydride)] as polymer backbone, chlorophyll derivatives(CpD) extracted from silkworm excreta as targeting moiety and 5‐fluorouracil and 6‐mercaptopurine as pharmacons were selected. The polymer exhibited an antitumor activity comparable to that of cyclophosphamide in vivo. CpD as well as CpD‐polymer conjugate were localized on tumor cells in vitro and delivered to tumor tissues in vivo specifically. The targeting polymeric antitumor agents were synthesized by coupling pharmacons and CpD on the polymer chain with the aid of reactions between functionalities of the reactants and anhydride groups on the polymer backbone. Various tests of their biological activities in vivo are in progress.
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