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New inhibitors of angiogenesis with antitumor activity in vivo.

Abstract：

:Angiogenesis is a requirement for the sustained growth and proliferation of solid tumors, and the development of new compounds that induce a sustained inhibition of the proangiogenic signaling generated by tumor hypoxia still remains as an important unmet need. In this work, we describe a new antiangiogenic compound (22) that inhibits proangiogenic signaling under hypoxic conditions in breast cancer cells. Compound 22 blocks the MAPK pathway, impairs cellular migration under hypoxic conditions, and regulates a set of genes related to angiogenesis. These responses are mediated by HIF-1α, since the effects of compound 22 mostly disappear when its expression is knocked-down. Furthermore, administration of compound 22 in a xenograft model of breast cancer produced tumor growth reductions ranging from 46 to 55% in 38% of the treated animals without causing any toxic side effects. Importantly, in the responding tumors, a significant reduction in the number of blood vessels was observed, further supporting the mechanism of action of the compound. These findings provide a rationale for the development of new antiangiogenic compounds that could eventually lead to new drugs suitable for the treatment of some types of tumors either alone or in combination with other agents.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Marín-Ramos NI,Alonso D,Ortega-Gutiérrez S,Ortega-Nogales FJ,Balabasquer M,Vázquez-Villa H,Andradas C,Blasco-Benito S,Pérez-Gómez E,Canales Á,Jiménez-Barbero J,Marquina A,del Prado JM,Sánchez C,Martín-Fontecha M,López-Rodrí

doi

10.1021/jm5019252

subject

Has Abstract

pub_date

2015-05-14 00:00:00

pages

3757-66

issue

9

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

杂志文章

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