A series of derivatives of the new ring system thiopyrano[2,3-e]indol-2-one was prepared with the aim of obtaining new photochemotherapeutic drugs. Biological screenings were performed on this new class of photoactivable drugs and a strong antiproliferative effect was observed upon irradiation with UVA light. The compound bearing a methyl substituent at the pyrrole nitrogen resulted as the most interesting showing IC50 in the nanomolar range.
BARRAJA P, SCIABICA L, DIANA P, LAURIA A, MONTALBANO A, ALMERICO AM, et al. (2005). SYNTHESIS AND PHOTOCHEMIOTHERAPEUTIC ACTIVITY OF THIOPYRANO[2,3-E]INDOL-2-ONES. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 15(9), 2291-2294 [10.1016/j.bmcl.2005.03.016].
SYNTHESIS AND PHOTOCHEMIOTHERAPEUTIC ACTIVITY OF THIOPYRANO[2,3-E]INDOL-2-ONES
BARRAJA, Paola;SCIABICA, Laura;DIANA, Patrizia;LAURIA, Antonino;MONTALBANO, Alessandra;ALMERICO, Anna Maria;DATTOLO, Gaetano;CIRRINCIONE, Girolamo;
2005-01-01
Abstract
A series of derivatives of the new ring system thiopyrano[2,3-e]indol-2-one was prepared with the aim of obtaining new photochemotherapeutic drugs. Biological screenings were performed on this new class of photoactivable drugs and a strong antiproliferative effect was observed upon irradiation with UVA light. The compound bearing a methyl substituent at the pyrrole nitrogen resulted as the most interesting showing IC50 in the nanomolar range.
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