Naphthalimido derivatives as antifolate thymidylate synthase inhibitors |
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| Authors: | MP Costi D Tondi M Rinaldi D Barlocco G Cignarella DV Santi C Musiu I Pudu G Vacca P La Colla |
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| Institution: | 1Dipartimento Scienze Farmaceutiche, Via Campi 183, 41100 Modena, Italy;2Istituto Chimica Farmaceutica e Tossicologica, Viale Abruzzi 42, 20131 Milan, Italy;3Department of Biochemistry and Biophysics, University of California, San Francisco, CA 94143, USA;4Dipartimento Biologia Sperimentale, Sez Microbiologia, Viale Regina Margherita 45, 09124 Cagliari, Italy |
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| 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. |
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| Keywords: | thymidylate synthase inhibition naphthalimido derivatives |
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