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Abstract
Abstract Antifolates are interfering specifically with DNA synthesis in the S-phase of the cell cycle. Thus, they are cytotoxic to rapidly dividing cancer cells, which replicate their DNA more frequently. Some antifolates bind with high affinity to the cell-membrane-associated folate receptor (FR). FR is frequently over-expressed in some of the most prevalent tumors. FR-binding antifolates can also be used as ligands for FR-targeted delivery of therapeutic agents. With this presentation we are reporting an improved synthesis of the FR-binding antifolate CB3717. Furthermore, to demonstrate its dual utility as FR-ligand and therapeutic agent, we designed and synthesized a conjugate of CB3717 with the highly cytotoxic agent Desacetylvinblastine Monohydrazide. A hydrophilic spacer unit and two biologically releasable disulfide-based linker systems were used to construct the conjugate. This conjugate exhibited high binding affinity for FR and excellent anti-tumor activity in vivo (subcutaneous FR+ KB tumors). Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 1929. doi:1538-7445.AM2012-1929
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