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KI1491PelitrexolQuoteQuote

Chemical Characteristic

Product NamePelitrexol
SynonymsAG2037
CAS No.446022-33-9
Molecular Weight 463.51
FormulaC20H25N5O6S
Chemical NameN-((5-(2-((6S)-2-Amino-1,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl)ethyl)-4-methyl-2-thienyl)carbonyl)-L-glutamic acid
SmilesC(=O)(C(NC(=O)c1cc(c(s1)CCC1Cc2c([nH]c(nc2=O)N)NC1)C)CCC(=O)O)O
Chemical Structure

Biological activities

Pelitrexol is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor. Pelitrexol inhibits activity of GARFT, which is the first folate-dependent enzyme of the de novo purine synthesis pathway essential for cell proliferation. Ultimately, Pelitrexol causes cell cycle arrest in S-phase and inhibits tumor cell proliferation.[1]

References

[1] Hu S, et al. Efficient chemoenzymatic synthesis of pelitrexol via enzymic differentiation of a remote stereocenter. Org Lett. 2006, 8(8): 1653-1655.

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