Antiproliferative activity of synthetic naphthoquinones related to lapachol. First synthesis of 5-hydroxylapachol |
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| Authors: | Evelyn L Bonifazi Carla Ríos-Luci Leticia G León Gerardo Burton José M Padrón Rosana I Misico |
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| Institution: | 1. Departamento de Química Orgánica and UMYMFOR (CONICET-UBA), Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón 2, Ciudad Universitaria, C1428EHA Buenos Aires, Argentina;2. Instituto Universitario de Bio-Orgánica Antonio González (IUBO-AG), Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain;3. BioLab, Instituto Canario de Investigación del Cáncer (ICIC), C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain |
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| Abstract: | A series of 5-hydroxy-1,4-naphthoquinones analogues was synthesized from juglone (6) and their antiproliferative activity against a representative panel of six human solid tumor cell lines has been investigated. The 2,5-dihydroxy-3-(3-methylbut-2-enyl)naphthalene-1,4-dione (4) and 2,3-dihydro-5-hydroxy-2-(prop-1-en-2-yl)naphtho2,3-b]furan-4,9-dione (27) were the most potent antiproliferative agents with GI50 values of 0.42–8.1 and 0.80–2.2 μM, respectively. The results provide insight into the correlation between some structural properties of 5-hydroxynaphthoquinones and their antiproliferative activity. |
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