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.

Naphthalimido Derivatives as Antifolate Thymidylate Synthase Inhibitors / Costi, Mp; Tondi, Donatella; Rinaldi, M; Barlocco, D; Cignarella, G; Santi, Dv; Musiu, C; Pudu, I; Vacca, G; Lacolla, P.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 31 (12):(1996), pp. 1011-1016. [10.1016/S0223-5234(97)86180-6]

Naphthalimido Derivatives as Antifolate Thymidylate Synthase Inhibitors

COSTI, MP;TONDI, Donatella;
1996

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.
31 (12)
1011
1016
Naphthalimido Derivatives as Antifolate Thymidylate Synthase Inhibitors / Costi, Mp; Tondi, Donatella; Rinaldi, M; Barlocco, D; Cignarella, G; Santi, Dv; Musiu, C; Pudu, I; Vacca, G; Lacolla, P.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 31 (12):(1996), pp. 1011-1016. [10.1016/S0223-5234(97)86180-6]
Costi, Mp; Tondi, Donatella; Rinaldi, M; Barlocco, D; Cignarella, G; Santi, Dv; Musiu, C; Pudu, I; Vacca, G; Lacolla, P.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/610099
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