Výsledky vyhledávání - "Mathew P, Leese"

Akademický článek

Accessing simply-substituted 4-hydroxytetrahydroisoquinolines via Pomeranz–Fritsch–Bobbitt reaction with non-activated and moderately-activated systems

Autor: Marco Mottinelli, Mathew P. Leese, Barry V. L. Potter

Publikováno v: Beilstein Journal of Organic Chemistry, Vol 13, Iss 1, Pp 1871-1878 (2017)

Background: 1,2,3,4-Tetrahydroisoquinolines (THIQs) are common motifs in alkaloids and in medicinal chemistry. Synthetic access to THIQs via the Pomeranz–Fritsch–Bobbit (PFB) methodology using mineral acids for deactivated, electron-poor aromatic

Externí odkaz: https://doaj.org/article/a1321fe5e52840bba90ef1c339f7ab6c

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N ‐Phenyl‐1,2,3,4‐tetrahydroisoquinoline: An Alternative Scaffold for the Design of 17β‐Hydroxysteroid Dehydrogenase 1 Inhibitors

Autor: Marco Mottinelli, Mathew P. Leese, Tea Lanišnik Rižner, Barry V. L. Potter, Maša Sinreih

Publikováno v: Potter, B, Mottinelli, M & Leese, M P 2021, ' N-Phenyl-1,2,3,4-tetrahydroisoquinoline: an alternative scaffold for design of 17-hydroxysteroid dehydrogenase 1 inhibitors ', ChemMedChem, vol. 16, no. 1, pp. 259-291 . https://doi.org/10.1002/cmdc.202000762

17β‐Hydroxysteroid dehydrogenases act at the pre‐receptor level, catalysing interconversion at the C17 position between oxidized and reduced forms of steroidal nuclear receptor ligands. The type 1 enzyme, expressed in malignant cells, catalyses

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76403185a747b5db1b1652df15b7eb65
https://doi.org/10.1002/cmdc.202000762

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Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure

Autor: Ernest Hamel, Pascoe Mannion, Grégory Menchon, Mathew P. Leese, Michel O. Steinmetz, Philip G. Kasprzyk, Mark P. Thomas, Eric Ferrandis, Barry V. L. Potter, Fabrice Jourdan, Paul A. Foster, Andrea E. Prota, Wolfgang Dohle

Publikováno v: Journal of Medicinal Chemistry. 61:1031-1044

Quinazolinone-based anti-cancer agents were designed, decorated with functional groups from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl sulfamate motif of steroid sulfatase (STS) inhibitors. The steroidal AB-ring s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66a2cfd9fa7b18e19c31a4bfb1e2c49f
https://doi.org/10.1021/acs.jmedchem.7b01474

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Targeted NF1 cancer therapeutics with multiple modes of action: small molecule hormone-like agents resembling the natural anticancer metabolite, 2-methoxyoestradiol

Autor: Mathew P. Leese, Yu Chi Shen, Daysha Ferrer-Torres, Kate F. Barald, Wolfgang Dohle, Ravi Upadhyayula, Tammy Hsia, Barry V. L. Potter, Stephanie Cevallos, Ryan J. Messick, Douglas M. Jewett, Therese M. Roth

Publikováno v: British Journal of Cancer

Background: Both the number and size of tumours in NF1 patients increase in response to the rise in steroid hormones seen at puberty and during pregnancy. The size of tumours decreases after delivery, suggesting that hormone-targeting therapy might p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b4288bf0d900ef0e86ae35fa044927f6
https://doi.org/10.1038/bjc.2015.345

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Synthesis, Antitubulin, and Antiproliferative SAR of C3/C1-Substituted Tetrahydroisoquinolines

Autor: Ernest Hamel, Ann Fiore, Simon P. Newman, Ruoli Bai, Mathew P. Leese, Meriel R. Major, Fabrice Jourdan, Philip G. Kasprzyk, Wolfgang Dohle, Eric Ferrandis, Atul Purohit, Barry V. L. Potter

Publikováno v: ChemMedChem. 9:350-370

The syntheses and antiproliferative activities of novel substituted tetrahydroisoquinoline derivatives and their sulfamates are discussed. Biasing of conformational populations through substitution on the tetrahydroisoquinoline core at C1 and C3 has

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4704a75c99b657f197a8b9002766f84c
https://doi.org/10.1002/cmdc.201300412

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Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors

Autor: Fabrice Jourdan, Eric Ferrandis, Meriel R. Kimberley, Ernest Hamel, Barry V. L. Potter, Ruoli Bai, Wolfgang Dohle, Mathew P. Leese, Mark P. Thomas

Publikováno v: ACS Medicinal Chemistry Letters

Structure–activity relationship translation offers an expeditious means for discovery of new active series. This approach was applied to discover tetrahydroisoquinoline (THIQ)-based steroidomimetic microtubule disruptors. The two A-ring elements of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cff378e055e453c0255790db93281078
https://doi.org/10.1021/ml200232c

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Structure–Activity Relationships of C-17-Substituted Estratriene-3-O-sulfamates as Anticancer Agents

Autor: Simon P. Newman, Fabrice Jourdan, Surinder K. Chander, Atul Purohit, Eric Ferrandis, Barry V. L. Potter, Wolfgang Dohle, Mathew P. Leese

Publikováno v: Journal of Medicinal Chemistry. 54:4863-4879

The synthesis and antiproliferative activities of analogues of 2-substituted estradiol-3,17-O,O-bis-sulfamates (E2bisMATEs) are discussed. Modifications of the C-17 substituent confirm that an H-bond acceptor is essential for high activity; its optim

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c81d2db41d81728733032b64f8149a47
https://doi.org/10.1021/jm200483x

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Synthesis, Antitubulin, and Antiproliferative SAR of Analogues of 2-Methoxyestradiol-3,17-O,O-bis-sulfamate

Autor: Simon P. Newman, Fabrice Jourdan, Barry V. L. Potter, Mathew P. Leese, Eric Ferrandis, Ernest Hamel, Atul Purohit, Wolfgang Dohle, Michael J. Reed

Publikováno v: Journal of Medicinal Chemistry. 53:2942-2951

The synthesis and antiproliferative activity of analogues of estradiol 3,17-O,O-bis-sulfamates (E2bisMATEs) are discussed. Modifications of the C-17 substituent reveal that an H-bond acceptor is essential for high antiproliferative activity. The loca

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b2d8de42356653eeea337adeff04475
https://doi.org/10.1021/jm9018806

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2-MeOE2bisMATE and 2-EtE2bisMATE induce cell cycle arrest and apoptosis in breast cancer xenografts as shown by a novel ex vivo technique

Autor: Atul Purohit, Paul A. Foster, Simon P. Newman, Y T Ho, Mathew P. Leese, Philip G. Kasprzyk, Barry V. L. Potter, Michael J. Reed

Publikováno v: Breast Cancer Research and Treatment. 111:251-260

Breast cancer is the leading cause of cancer deaths among women worldwide. The theory of targeting both cancer cells directly and their blood supply has significant therapeutic potential. However, to date, there are few clinically successful single a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::437da25a3d735adcb00e42a90dc5b2bb
https://doi.org/10.1007/s10549-007-9791-5

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In vivo inhibition of angiogenesis by sulphamoylated derivatives of 2-methoxyoestradiol

Autor: Surinder K. Chander, Michael J. Reed, Mathew P. Leese, A. Purohit, Paul A. Foster, Barry V. L. Potter, Simon P. Newman

Publikováno v: British Journal of Cancer

Drugs that inhibit growth of tumours and their blood supply could have considerable therapeutic potential. 2-Methoxyoestradiol-3,17-O,O-bis-sulphamate (2-MeOE2bisMATE) has been shown to inhibit the proliferation of MCF-7 (ER+) breast cancer cells and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::692fd9c5504169b1057e9269dd3db90c
https://doi.org/10.1038/sj.bjc.6603727

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