The α-FR has been reported to be overexpressed in many carcinomas, in particular those of the ovary and uterus. The high expression of α-FR in some tumours compared with normal tissues has been exploited over the last decade for folate-mediated targeting of macromolecules, anticancer drugs, imaging agents and nucleic acids to cancer cells. CB300638, a cyclopenta [g] quinazoline-based inhibitor of thymidylate synthase (TS), has ...
