Methoxy and bromo scans on N-(5-methoxyphenyl) methoxybenzenesulphonamides reveal potent cytotoxic compounds, especially against the human breast adenocarcinoma MCF7 cell line

Autor: Myriam González, María Ovejero-Sánchez, Alba Vicente-Blázquez, Manuel Medarde, Rogelio González-Sarmiento, Rafael Peláez

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 1029-1047 (2021)

Thirty seven N-(5-methoxyphenyl)-4-methoxybenzenesulphonamide with methoxy or/and bromo substitutions (series 1-4) and with different substituents on the sulphonamide nitrogen have been synthesised. 21 showed sub-micromolar cytotoxicity against HeLa

Externí odkaz: https://doaj.org/article/ed4db40aad264714b3a1ccaddd495c19

New diarylsulfonamide inhibitors of Leishmania infantum amastigotes

Autor: Rafael Peláez, Raquel Álvarez, M. González, Manuel Medarde, Vicente Larraga, Pedro J. Alcolea

Publikováno v: International Journal for Parasitology: Drugs and Drug Resistance, Vol 16, Iss, Pp 45-64 (2021)
Digital.CSIC. Repositorio Institucional del CSIC
instname
GREDOS. Repositorio Institucional de la Universidad de Salamanca
Digital.CSIC: Repositorio Institucional del CSIC
Consejo Superior de Investigaciones Científicas (CSIC)
International Journal for Parasitology: Drugs and Drug Resistance

20 p.-7 fig.-1 tab.
New drugs against visceral leishmaniasis with mechanisms of action differing from existing treatments and with adequate cost, stability, and properties are urgently needed. No antitubulin drug is currently in the clinic again

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4fdfd4ab4cbf19d82836e3adc8372c7
http://www.sciencedirect.com/science/article/pii/S2211320721000099

Novel amino analogs of the trimethoxyphenyl ring in potent colchicine site ligands improve solubility by the masked polar group incorporation (MPGI) strategy

Autor: Myriam, González, Younes, Ellahioui, Laura, Gallego, Alba, Vicente-Blázquez, Raquel, Álvarez, Manuel, Medarde, Rafael, Peláez

Publikováno v: Bioorganic Chemistry. 131:106282

The low aqueous solubility of colchicine site antimitotic agents, of which the trimethoxyphenyl (A ring) is a heavy contributor, is a serious drawback in their clinical development. We have designed new A ring analogs with chameleonic masked polar am

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ddd5f2e7eaf1e81ce562b5868542dcf5
https://doi.org/10.1016/j.bioorg.2022.106282

Physiological characteristics of allo-cholic acid1

Autor: Maria E. Mendoza, Maria J. Monte, Maria A. Serrano, Marçal Pastor-Anglada, Bruno Stieger, Peter J. Meier, Manuel Medarde, Jose J.G. Marin

Publikováno v: Journal of Lipid Research, Vol 44, Iss 1, Pp 84-92 (2003)

The physiological characterstics of allo-cholic acid (A91), a typically fetal bile acid that reappears during liver regeneration and carcinogenesis were investigated. [14C] Tauro-ACA (TACA) uptake by Chinese hamster ovary cells expressing rat organic

Externí odkaz: https://doaj.org/article/40e47fecdc5840029f87cb4fe7e9b0b7

Microtubule Destabilizing Sulfonamides as An Alternative to Taxane-Based Chemotherapy

Autor: Ana B. Herrero, Raquel Álvarez, Rafael Peláez, M. González, Manuel Medarde, Alba Vicente-Blázquez, María Ovejero-Sánchez, Rogelio González-Sarmiento

Publikováno v: International Journal of Molecular Sciences
Volume 22
Issue 4
GREDOS. Repositorio Institucional de la Universidad de Salamanca
Fundacion Sancho el Sabio Fundazioa (FSS)
International Journal of Molecular Sciences, Vol 22, Iss 1907, p 1907 (2021)
Digital.CSIC. Repositorio Institucional del CSIC
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© 2021 by the authors.
Pan-Gyn cancers entail 1 in 5 cancer cases worldwide, breast cancer being the most commonly diagnosed and responsible for most cancer deaths in women. The high incidence and mortality of these malignancies, together with

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e5490819af61bff0d02c13c745ae14fe