Literature DB >> 16455256

Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds.

S D Guile1, J R Bantick, D R Cheshire, M E Cooper, A M Davis, D K Donald, R Evans, C Eyssade, D D Ferguson, S Hill, R Hutchinson, A H Ingall, L P Kingston, I Martin, B P Martin, R T Mohammed, C Murray, M W D Perry, R H Reynolds, P V Thorne, D J Wilkinson, J Withnall.   

Abstract

A novel series of potent blockers of the monocarboxylate transporter, MCT1, is disclosed. From very potent but lipophilic lead compounds, systematic changes to all parts of the molecule, targeting reduction in log D, afforded compounds with significantly improved overall properties. These compounds show potent immunomodulatory activity.

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Year:  2006        PMID: 16455256     DOI: 10.1016/j.bmcl.2006.01.024

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  16 in total

1.  In Vitro and In Vivo Efficacy of AZD3965 and Alpha-Cyano-4-Hydroxycinnamic Acid in the Murine 4T1 Breast Tumor Model.

Authors:  Xiaowen Guan; Marilyn E Morris
Journal:  AAPS J       Date:  2020-06-11       Impact factor: 4.009

2.  Preparation of tetrasubstituted pyrimido[4,5-d]pyrimidine diones.

Authors:  Hui Wang; Chao Wang; Thomas D Bannister
Journal:  Tetrahedron Lett       Date:  2015-04-08       Impact factor: 2.415

3.  MCT1 Modulates Cancer Cell Pyruvate Export and Growth of Tumors that Co-express MCT1 and MCT4.

Authors:  Candice Sun Hong; Nicholas A Graham; Wen Gu; Carolina Espindola Camacho; Vei Mah; Erin L Maresh; Mohammed Alavi; Lora Bagryanova; Pascal A L Krotee; Brian K Gardner; Iman Saramipoor Behbahan; Steve Horvath; David Chia; Ingo K Mellinghoff; Sara A Hurvitz; Steven M Dubinett; Susan E Critchlow; Siavash K Kurdistani; Lee Goodglick; Daniel Braas; Thomas G Graeber; Heather R Christofk
Journal:  Cell Rep       Date:  2016-02-11       Impact factor: 9.423

Review 4.  Anticancer agents that counteract tumor glycolysis.

Authors:  Carlotta Granchi; Filippo Minutolo
Journal:  ChemMedChem       Date:  2012-06-08       Impact factor: 3.466

Review 5.  Short-Chain Fatty Acid Transporters: Role in Colonic Homeostasis.

Authors:  Sathish Sivaprakasam; Yangzom D Bhutia; Shengping Yang; Vadivel Ganapathy
Journal:  Compr Physiol       Date:  2017-12-12       Impact factor: 9.090

6.  The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein.

Authors:  Matthew J Ovens; Christine Manoharan; Marieangela C Wilson; Clarey M Murray; Andrew P Halestrap
Journal:  Biochem J       Date:  2010-10-15       Impact factor: 3.857

7.  One-pot directed alkylation/deprotection strategy for the synthesis of substituted pyrrole[3,4-d]pyridazinones.

Authors:  Reji N Nair; Thomas D Bannister
Journal:  European J Org Chem       Date:  2015-03

8.  Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors.

Authors:  Reji N Nair; Jitendra K Mishra; Fangzheng Li; Mariola Tortosa; Chunying Yang; Joanne R Doherty; Michael Cameron; John L Cleveland; William R Roush; Thomas D Bannister
Journal:  Medchemcomm       Date:  2016-02-23       Impact factor: 3.597

9.  Pharmacokinetics of the Monocarboxylate Transporter 1 Inhibitor AZD3965 in Mice: Potential Enterohepatic Circulation and Target-Mediated Disposition.

Authors:  Xiaowen Guan; Marilyn E Morris
Journal:  Pharm Res       Date:  2019-12-10       Impact factor: 4.200

10.  AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10.

Authors:  Matthew J Ovens; Andrew J Davies; Marieangela C Wilson; Clare M Murray; Andrew P Halestrap
Journal:  Biochem J       Date:  2010-01-15       Impact factor: 3.857

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