PAMAM dendrimer has been studied as a macromolecular carrier to deliver drug resulting in accumulation within the tumor tissue due to EPR effect. By applying its derivatives with cleavable cystamine core, different half dendrons covalently modified with different functionalities could be assembled into one conjugate. It is also reported that vitamin receptors are over-expressed in various tumor cell lines. To exploit these favorable properties, a novel asymmetrical bow-tie PAMAM dendrimer-based conjugate through a bis-(imido)-alkene linking a vitamin, a second generation taxoid (SB-T-1214), a fluorescent probe and a disulfide linker was designed and synthesized. The synthesis and biological evaluation of the novel dendrimer-based drug conjugate will be presented.

Synthesis of a novel asymmetrical bow-tie PAMAM dendrimer-based drug conjugate bearing biotin and a second-generation taxoid

244th National Meeting (2012)

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