Raltitrexed | Thymidylate synthase inhibitor

Raltitrexed chemical structure Focus Biomolecules

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Raltitrexed (112887-68-0) is an inhibitor of thymidylate synthase with significantly increased potency in many cancer cell lines when compared with 5-fluorouracil.1,2  It is also an inhibitor of the methyltransferase G9a (IC50 = 120 nM) and decreased Aß aggregates in C. elegans indicating therapeutic potential for the treatment of Alzheimer’s disease.3

References/Citations:

  1. Marsham et al. (1991) Quinazoline Antifolate Thymidylate Synthase Inhibitors: Heterocyclic Benzoyl Ring Modifications; J.  Med. Chem. 34 1594
  2. Jackman et al. (1995) ZD1694(Tomudex): A New Thymidylate Synthase Inhibitor with Activity in Colorectal Cancer; Eur. J. Cancer 31A 1277
  3. Jana et al. (2023) Repurposing of Raltitrexed as an Effective G91/EHMT2 Inhibitor and Promising Anti-Alzheimer’s Agent; ACS Med. Chem. Lett. 14 1531
112887-68-0, ICI D 1694, Raltitrexed, Raltitrexed supplier, Thymidylate synthase inhibitor, ZD1694
Alternate Name:
ICI D 1694; ZD1694

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Raltitrexed (112887-68-0) is an inhibitor of thymidylate synthase with significantly increased potency in many cancer cell lines when compared with 5-fluorouracil.1,2  It is also an inhibitor of the methyltransferase G9a (IC50 = 120 nM) and decreased Aß aggregates in C. elegans indicating therapeutic potential for the treatment of Alzheimer’s disease.3

References/Citations:

  1. Marsham et al. (1991) Quinazoline Antifolate Thymidylate Synthase Inhibitors: Heterocyclic Benzoyl Ring Modifications; J.  Med. Chem. 34 1594
  2. Jackman et al. (1995) ZD1694(Tomudex): A New Thymidylate Synthase Inhibitor with Activity in Colorectal Cancer; Eur. J. Cancer 31A 1277
  3. Jana et al. (2023) Repurposing of Raltitrexed as an Effective G91/EHMT2 Inhibitor and Promising Anti-Alzheimer’s Agent; ACS Med. Chem. Lett. 14 1531