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Prospective study directed to the synthesis of unsymmetrical linked bis-5-arylidene rhodanine derivatives via “one-pot two steps” reactions under microwave irradiation with their antitumor activity

Abstract : We here report on the synthesis of new unsymmetrical linked bis-5-arylidene rhodanine derivatives with stereocontrolled Z-configuration. The 6 steps synthesis was achieved and the key steps are the construction of the two 5-arylidene rhodanine moieties using an “one-pot two-steps” method under microwave dielectric heating in a closed reactor. The intermediates 6, 7 and desired unsymmetrical compounds 9 have been also evaluated for their in vitro inhibition of cell proliferation (Huh7 D12, Caco2, MDA-MB 231, HCT116, and NCI-H727 tumoral cell lines). Two of all compounds have shown potent activity against Huh7 D12, Caco2, and MDA-MB 231.
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https://hal-univ-rennes1.archives-ouvertes.fr/hal-01114518
Contributor : Laurent Jonchère <>
Submitted on : Monday, February 9, 2015 - 3:21:16 PM
Last modification on : Saturday, October 24, 2020 - 3:40:30 AM

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Wacothon Karime Coulibaly, Ludovic Paquin, Anoubilé Bénie, Yves-Alain Békro, Rémy Le Guével, et al.. Prospective study directed to the synthesis of unsymmetrical linked bis-5-arylidene rhodanine derivatives via “one-pot two steps” reactions under microwave irradiation with their antitumor activity. Medicinal Chemistry Research, Springer Verlag, 2015, 24 (4), pp.1653-1661. ⟨10.1007/s00044-014-1186-7⟩. ⟨hal-01114518⟩

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