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Items: 1 to 20 of 21

1.

The 3S Enantiomer Drives Enolase Inhibitory Activity in SF2312 and Its Analogues.

Pisaneschi F, Lin YH, Leonard PG, Satani N, Yan VC, Hammoudi N, Raghavan S, Link TM, K Georgiou D, Czako B, Muller FL.

Molecules. 2019 Jul 9;24(13). pii: E2510. doi: 10.3390/molecules24132510.

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Development and validation of chemical features-based proton-coupled folate transporter/activity and reduced folate carrier/activity models (pharmacophores).

Shah K, Raghavan S, Hou Z, Matherly LH, Gangjee A.

J Mol Graph Model. 2018 May;81:125-133. doi: 10.1016/j.jmgm.2018.02.007. Epub 2018 Feb 20.

4.

ENOblock Does Not Inhibit the Activity of the Glycolytic Enzyme Enolase.

Satani N, Lin YH, Hammoudi N, Raghavan S, Georgiou DK, Muller FL.

PLoS One. 2016 Dec 28;11(12):e0168739. doi: 10.1371/journal.pone.0168739. eCollection 2016.

5.

Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis.

Golani LK, Wallace-Povirk A, Deis SM, Wong J, Ke J, Gu X, Raghavan S, Wilson MR, Li X, Polin L, de Waal PW, White K, Kushner J, O'Connor C, Hou Z, Xu HE, Melcher K, Dann CE 3rd, Matherly LH, Gangjee A.

J Med Chem. 2016 Sep 8;59(17):7856-76. doi: 10.1021/acs.jmedchem.6b00594. Epub 2016 Aug 26.

6.

Correction to Structure-Activity Profiles of Novel 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Antifolates with Modified Amino Acids for Cellular Uptake by Folate Receptors α and β and the Proton-Coupled Folate Transporter.

Golani LK, George C, Zhao S, Raghavan S, Orr S, Wallace A, Wilson MR, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2016 Apr 28;59(8):4032. doi: 10.1021/acs.jmedchem.6b00502. Epub 2016 Apr 15. No abstract available.

7.

6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors.

Wang L, Wallace A, Raghavan S, Deis SM, Wilson MR, Yang S, Polin L, White K, Kushner J, Orr S, George C, O'Connor C, Hou Z, Mitchell-Ryan S, Dann CE 3rd, Matherly LH, Gangjee A.

J Med Chem. 2015 Sep 10;58(17):6938-59. doi: 10.1021/acs.jmedchem.5b00801. Epub 2015 Aug 28.

8.

The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.

Zhang X, Raghavan S, Ihnat M, Hamel E, Zammiello C, Bastian A, Mooberry SL, Gangjee A.

Bioorg Med Chem. 2015 May 15;23(10):2408-23. doi: 10.1016/j.bmc.2015.03.061. Epub 2015 Mar 30.

9.

Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents.

Wang Y, Mitchell-Ryan S, Raghavan S, George C, Orr S, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2015 Feb 12;58(3):1479-93. doi: 10.1021/jm501787c. Epub 2015 Feb 2.

10.

Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors α and β and the proton-coupled folate transporter.

Golani LK, George C, Zhao S, Raghavan S, Orr S, Wallace A, Wilson MR, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2014 Oct 9;57(19):8152-66. doi: 10.1021/jm501113m. Epub 2014 Sep 19. Erratum in: J Med Chem. 2016 Apr 28;59(8):4032.

11.

The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.

Zhang X, Raghavan S, Ihnat M, Thorpe JE, Disch BC, Bastian A, Bailey-Downs LC, Dybdal-Hargreaves NF, Rohena CC, Hamel E, Mooberry SL, Gangjee A.

Bioorg Med Chem. 2014 Jul 15;22(14):3753-72. doi: 10.1016/j.bmc.2014.04.049. Epub 2014 May 14.

13.

Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor α and inhibition of de novo purine nucleotide biosynthesis.

Wang Y, Cherian C, Orr S, Mitchell-Ryan S, Hou Z, Raghavan S, Matherly LH, Gangjee A.

J Med Chem. 2013 Nov 14;56(21):8684-95. doi: 10.1021/jm401139z. Epub 2013 Oct 30.

15.

Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.

Gangjee A, Namjoshi OA, Raghavan S, Queener SF, Kisliuk RL, Cody V.

J Med Chem. 2013 Jun 13;56(11):4422-41. doi: 10.1021/jm400086g. Epub 2013 May 21.

16.

Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.

Gangjee A, Zaware N, Raghavan S, Disch BC, Thorpe JE, Bastian A, Ihnat MA.

Bioorg Med Chem. 2013 Apr 1;21(7):1857-64. doi: 10.1016/j.bmc.2013.01.040. Epub 2013 Jan 31.

17.

Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.

Gangjee A, Zaware N, Devambatla RK, Raghavan S, Westbrook CD, Dybdal-Hargreaves NF, Hamel E, Mooberry SL.

Bioorg Med Chem. 2013 Feb 15;21(4):891-902. doi: 10.1016/j.bmc.2012.12.010. Epub 2012 Dec 20.

18.

N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.

Gangjee A, Zaware N, Raghavan S, Yang J, Thorpe JE, Ihnat MA.

Bioorg Med Chem. 2012 Apr 1;20(7):2444-54. doi: 10.1016/j.bmc.2012.01.029. Epub 2012 Feb 4.

19.

Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.

Gangjee A, Zhao Y, Lin L, Raghavan S, Roberts EG, Risinger AL, Hamel E, Mooberry SL.

J Med Chem. 2010 Nov 25;53(22):8116-28. doi: 10.1021/jm101010n. Epub 2010 Oct 25. Erratum in: J Med Chem. 2011 Feb 10;54(3):913.

20.

Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.

Gangjee A, Zhao Y, Raghavan S, Ihnat MA, Disch BC.

Bioorg Med Chem. 2010 Jul 15;18(14):5261-73. doi: 10.1016/j.bmc.2010.05.049. Epub 2010 May 25.

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