Synthesis and anticancer activity evaluation of 2(4-alkoxyphenyl)cyclopropyl hydrazides and triazolo phthalazines |
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| Authors: | Prithwiraj De Michel Baltas Delphine Lamoral-Theys Céline Bruyère Robert Kiss Florence Bedos-Belval Nathalie Saffon |
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| Institution: | 1. Université de Toulouse, UPS, LSPCMIB (Laboratoire de Synthèse et Physico-Chimie de Molécules d’Intérêt Biologique), 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France;2. CNRS, LSPCMIB (Laboratoire de Synthèse et Physico-Chimie de Molécules d’Intérêt Biologique), 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France;3. Laboratoire de Chimie Analytique, Toxicologie et Chimie Physique Appliquée, Institut de Pharmacie, Université Libre de Bruxelles, Boulevard du Triomphe, 1050 Bruxelles, Belgique;4. Laboratoire de Toxicologie, Institut de Pharmacie, Université Libre de Bruxelles, Boulevard du Triomphe, 1050 Bruxelles, Belgique;5. Université de Toulouse, UPS, Structure Fédérative Toulousaine en Chimie Moléculaire, FR 2599, 118, Route de Narbonne, F-31062 Toulouse Cedex 9, France |
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| Abstract: | A series of new 2(4-alkoxyphenyl)cyclopropyl hydrazide- and triazolo-derivatives were synthesized starting from 4-hydroxycinnamic acid (1) in a clean, mild, efficient and straightforward synthetic protocol. These compounds consisting of different alkoxy substitution, phenylcyclopropyl backbone and different heterocyclic groups were evaluated for in vitro anticancer activity against 4 cell lines displaying certain levels of resistance to pro-apoptotic stimuli and 2 cell lines sensitive to pro-apoptotic compounds. Compounds 7f and 8e were most active and displaying moderate in vitro cytostatic effect through different mechanisms. Significantly, chemically modified derivatives could be obtained in order to develop novel types of compounds aiming to combat apoptosis-resistant cancers, for example, those cancers associated with dismal prognoses. |
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