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Targeted Dendrimeric Anticancer Prodrug: A Methotrexate-Folic Acid-Poly(amidoamine) Conjugate and a Novel, Rapid, “One Pot” Synthetic Approach

✍ Scribed by Zhang, Yuehua; Thomas, Thommey P.; Desai, Ankur; Zong, Hong; Leroueil, Pascale R.; Majoros, Istvan J.; Baker, James R.


Book ID
127051557
Publisher
American Chemical Society
Year
2010
Tongue
English
Weight
724 KB
Volume
21
Category
Article
ISSN
1043-1802

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✦ Synopsis


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.


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