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Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transporter for cellular entry.
Deng Y, Zhou X, Kugel Desmoulin S, Wu J, Cherian C, Hou Z, Matherly LH, Gangjee A. Deng Y, et al. Among authors: gangjee a. J Med Chem. 2009 May 14;52(9):2940-51. doi: 10.1021/jm8011323. J Med Chem. 2009. PMID: 19371039 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: gangjee a. 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. Among authors: gangjee a. 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.
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: gangjee a. 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.
Therapeutic targeting of a novel 6-substituted pyrrolo [2,3-d]pyrimidine thienoyl antifolate to human solid tumors based on selective uptake by the proton-coupled folate transporter.
Kugel Desmoulin S, Wang L, Hales E, Polin L, White K, Kushner J, Stout M, Hou Z, Cherian C, Gangjee A, Matherly LH. Kugel Desmoulin S, et al. Among authors: gangjee a. Mol Pharmacol. 2011 Dec;80(6):1096-107. doi: 10.1124/mol.111.073833. Epub 2011 Sep 22. Mol Pharmacol. 2011. PMID: 21940787 Free PMC article.
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. Among authors: gangjee a. 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.
Intestinal transport of aminopterin enantiomers in dogs and humans with psoriasis is stereoselective: evidence for a mechanism involving the proton-coupled folate transporter.
Menter A, Thrash B, Cherian C, Matherly LH, Wang L, Gangjee A, Morgan JR, Maeda DY, Schuler AD, Kahn SJ, Zebala JA. Menter A, et al. Among authors: gangjee a. J Pharmacol Exp Ther. 2012 Sep;342(3):696-708. doi: 10.1124/jpet.112.195479. Epub 2012 May 31. J Pharmacol Exp Ther. 2012. PMID: 22653877 Free PMC article. Clinical Trial.
167 results