Data di Pubblicazione:
1996
Citazione:
Naphthalimido derivatives as antifolate thymidylate synthase inhibitors / M.P. Costi, D. Tondi, M. Rinaldi, D. Barlocco, G. Cignarella, D.V. Santi, C. Musiu, I. Pudu, G. Vacca, P. La Colla. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 31:12(1996), pp. 1011-1016.
Abstract:
A new series of N-(substituted)benzyl-1,8-naphthalimides 4, structurally related to the previously reported thymidylate synthase (TS) inhibitor naphthaleins 3, were synthesized and compounds tested for their inhibition of several species of TS. Moreover, their in vitro cytotoxicity together with antimycotic and antibacterial properties were assayed. While no activity was detected in the antibacterial tests, the m-nitro (4ae) and the p-nitro (4af) derivatives were found able to partially inhibit TS at low micromolar concentrations. Introduction of nitro or (substituted)-amino groups in position 4 of the naphthalic ring always led to less active compounds.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Inhibition; Naphthalimido derivatives; Thymidylate synthase
Elenco autori:
M.P. Costi, D. Tondi, M. Rinaldi, D. Barlocco, G. Cignarella, D.V. Santi, C. Musiu, I. Pudu, G. Vacca, P. La Colla
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