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Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase.
Wang L, Desmoulin SK, Cherian C, Polin L, White K, Kushner J, Fulterer A, Chang MH, Mitchell-Ryan S, Stout M, Romero MF, Hou Z, Matherly LH, Gangjee A. Wang L, et al. Among authors: desmoulin sk. J Med Chem. 2011 Oct 27;54(20):7150-64. doi: 10.1021/jm200739e. Epub 2011 Sep 22. J Med Chem. 2011. PMID: 21879757 Free PMC article.
Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry.
Wang L, Cherian C, Desmoulin SK, Polin L, Deng Y, Wu J, Hou Z, White K, Kushner J, Matherly LH, Gangjee A. Wang L, et al. Among authors: desmoulin sk. J Med Chem. 2010 Feb 11;53(3):1306-18. doi: 10.1021/jm9015729. J Med Chem. 2010. PMID: 20085328 Free PMC article.
Targeting the proton-coupled folate transporter for selective delivery of 6-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors of de novo purine biosynthesis in the chemotherapy of solid tumors.
Desmoulin SK, Wang Y, Wu J, Stout M, Hou Z, Fulterer A, Chang MH, Romero MF, Cherian C, Gangjee A, Matherly LH. Desmoulin SK, et al. Mol Pharmacol. 2010 Oct;78(4):577-87. doi: 10.1124/mol.110.065896. Epub 2010 Jul 2. Mol Pharmacol. 2010. PMID: 20601456 Free PMC article.