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Synthesis and biological activity of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl regioisomers as inhibitors of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier.
Wang L, Cherian C, Kugel Desmoulin S, Mitchell-Ryan S, Hou Z, Matherly LH, Gangjee A. Wang L, et al. J Med Chem. 2012 Feb 23;55(4):1758-70. doi: 10.1021/jm201688n. Epub 2012 Feb 3. J Med Chem. 2012. PMID: 22243528 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. J Med Chem. 2010 Feb 11;53(3):1306-18. doi: 10.1021/jm9015729. J Med Chem. 2010. PMID: 20085328 Free PMC article.
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. 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.