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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 · 2017

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.

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Antitumor and antiangiogenic potential of solomonamide synthesis intermediates

Author: 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
Year: 2017
Source: https://riuma.uma.es/xmlui/bitstream/10630/14768/1/Abstract%20P02-41.pdf
8/11/17 13'13
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FEBS3 Ba celona 2017
1s Join Mee ing on he F ench-Po uguese-Spanish
Biochemical and Molecula Biology Socie ies
Ba celona, 23 d – 26 h Oc obe
P02-41
An i umo and an iangiogenic po en ial o solomonamide syn hesis in e media es
Paloma Ca illo1, I án Cheng-Sánchez2, Mª Ca men Ocaña1, Bea iz Ma ínez-Po eda1, Miguel
Ángel Medina3, F ancisco Sa abia2, Ana R. Quesada3
1Uni e sidad de Málaga, Andalucía Tech, Depa amen o Biología Molecula y Bioquímica, Facul ad
de Ciencias e IBIMA, Málaga, ES, 2Uni e sidad de Málaga, Andalucía Tech, Depa amen o de
Química O gánica, Facul ad de Ciencias, Málaga, ES, 3Uni e sidad de Málaga, Andalucía Tech,
Depa amen o Biología Molecula y Bioquímica, Facul ad de Ciencias e IBIMA y U741
(CB06/07/0046) CIBER de En e medades Ra as, Málaga, ES
In his wo k we de eloped a new syn he ic s a egy owa ds he solomonamides. a no el class o
cyclopep ides o ma ine o igin. The desc ibed syn he ic app oach u ilized an ole in me a hesis eac ion
o o m he [15]-membe ed ing con ained in hese na u al p oduc s. Du ing he syn he ic p ocess, a
di e se se o analogues was gene a ed and we e alua ed hei po en ial an i umo ac i i y in i o. Fo
his pu pose we pe o med in i o p oli e a ion assays, de e mining he IC50 alues o he compounds
in a panel o umo cell lines. In addi ion, we e alua ed he possible an iangiogenic e ec s o hese
solomonamide analogues by using in i o endo helial cell di e en ia ion assays. Ou esul s showed
ha he po en ial an i umo and an iangiogenic ac i i y o he s udied analogues depended on hei
chemical s uc u e, sugges ing ha he p esence o speci ic unc ional g oups could be esponsible o
hei biological ac i i y. Fu he s udies a e needed o unde s and he basis o he obse ed ac i i ies in
endo helial and umo cells.
Ou expe imen al wo k is suppo ed by g an s BIO2014-56092-R (MINECO and FEDER) and
P12-CTS-1507 (Andalusian Go e nmen and FEDER) and unds om g oup BIO-267
(Andalusian Go e nmen ). The "CIBER de En e medades Ra as" is an ini ia i e om he ISCIII
(Spain). This communicac ion has he suppo o a a el g an "Uni e sidad de Málaga. Campus
de Excelencia In e nacional Andalucía Tech"