Antitumor and antiangiogenic potential of solomonamide synthesis intermediates
Carrillo Fernández, Paloma,Cheng-Sánchez, Iván,Ocaña Farfán, María del Carmen,Martínez-Póveda, Beatriz Amparo,Medina-Torres, Miguel Ángel,Sarabia-García, Francisco Ramón,Rodríguez-Quesada, Ana María
- Published
- 2017-11-09
- Language
- en
Abstract
In this work we developed a new synthetic strategy towards the solomonamides. a novel class of cyclopeptides of marine origin. The described synthetic approach utilized an olefin metathesis reaction to form the [15]-membered ring contained in these natural products. During the synthetic process, a diverse set of analogues was generated and we evaluated their potential antitumor activity in vitro. For this purpose we performed in vitro proliferation assays, determining the IC50 values of the compounds in a panel of tumor cell lines. In addition, we evaluated the possible antiangiogenic effects of these solomonamide analogues by using in vitro endothelial cell differentiation assays. Our results showed that the potential antitumor and antiangiogenic activity of the studied analogues depended on their chemical structure, suggesting that the presence of specific functional groups could be responsible of their biological activity. Further studies are needed to understand the basis of the observed activities in endothelial and tumor cells.
Full text
8/11/17 13'13 Página 1 de 1about:blank FEBS3 Barcelona 2017 1st Joint Meeting on the French-Portuguese-Spanish Biochemical and Molecular Biology Societies Barcelona, 23rd – 26th October P02-41 Antitumor and antiangiogenic potential of solomonamide synthesis intermediates Paloma Carrillo1, Iván Cheng-Sánchez2, Mª Carmen Ocaña1, Beatriz Martínez-Poveda1, Miguel Ángel Medina3, Francisco Sarabia2, Ana R. Quesada3 1Universidad de Málaga, Andalucía Tech, Departamento Biología Molecular y Bioquímica, Facultad de Ciencias e IBIMA, Málaga, ES, 2Universidad de Málaga, Andalucía Tech, Departamento de Química Orgánica, Facultad de Ciencias, Málaga, ES, 3Universidad de Málaga, Andalucía Tech, Departamento Biología Molecular y Bioquímica, Facultad de Ciencias e IBIMA y U741 (CB06/07/0046) CIBER de Enfermedades Raras, Málaga, ES In this work we developed a new synthetic strategy towards the solomonamides. a novel class of cyclopeptides of marine origin. The described synthetic approach utilized an olefin metathesis reaction to form the [15]-membered ring contained in these natural products. During the synthetic process, a diverse set of analogues was generated and we evaluated their potential antitumor activity in vitro. For this purpose we performed in vitro proliferation assays, determining the IC50 values of the compounds in a panel of tumor cell lines. In addition, we evaluated the possible antiangiogenic effects of these solomonamide analogues by using in vitro endothelial cell differentiation assays. Our results showed that the potential antitumor and antiangiogenic activity of the studied analogues depended on their chemical structure, suggesting that the presence of specific functional groups could be responsible of their biological activity. Further studies are needed to understand the basis of the observed activities in endothelial and tumor cells. Our experimental work is supported by grants BIO2014-56092-R (MINECO and FEDER) and P12-CTS-1507 (Andalusian Government and FEDER) and funds from group BIO-267 (Andalusian Government). The "CIBER de Enfermedades Raras" is an initiative from the ISCIII (Spain). This communicaction has the support of a travel grant "Universidad de Málaga. Campus de Excelencia Internacional Andalucía Tech"