| Literature DB >> 20128612 |
Yuehua Zhang1, Thommey P Thomas, Ankur Desai, Hong Zong, Pascale R Leroueil, Istvan J Majoros, James R Baker.
Abstract
A targeted dendrimeric anticancer prodrug, a conjugate of generation 5 (G5) polyamidoamine (PAMAM) dendrimer, folic acid (FA), and methotrexate (MTX), has been successfully synthesized by using a novel "one pot" approach which is simple, reproducible, and feasible for large-scale synthesis. All dendrimer products have been characterized by (1)H NMR, MALDI-TOF, GPC, and HPLC. With this new method, the ratio of FA versus MTX attached to the dendrimer can be easily tuned to achieve the desired therapeutic effect. A new analytical approach for calculating the numbers of FA and MTX attached to the dendrimer has been established. In vitro studies performed on FA receptor-expressing KB cells show that the new conjugate has a similar affinity and cytotoxic potency to G5-FA-MTX synthesized using the traditional multiple-step approach.Entities:
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Year: 2010 PMID: 20128612 PMCID: PMC2892195 DOI: 10.1021/bc9003958
Source DB: PubMed Journal: Bioconjug Chem ISSN: 1043-1802 Impact factor: 4.774