40118-17-0Relevant academic research and scientific papers
Synthesis of 1,3-benzodioxole derivatives containing a amino acid moiety in side chain
Leite, Ana Cristina Lima,Da Silva, Kezia Peixoto,Brondani, Dalci Jose
, p. 555 - 558 (2001)
The synthesis of the new amino-acyl derivatives starting from a 1,3-benzodioxole unit present in safrole is described. All the synthesised compounds, that could be conveniently prepared in a few steps process, have been characterised by the IR and the 1H-NMR Spectroscopy.
Synthesis, antitumour and antimicrobial activities of new peptidyl derivatives containing the 1,3-benzodioxole system
Leite, Ana Cristina Lima,Peixoto Da Silva, Kezia,De Souza, Ivone A.,Magali De Araújo, Janete,Brondani, Dalci José
, p. 1059 - 1065 (2004)
Two series of 5 and 6-substituted 1,3-benzodioxole peptidyl derivatives were synthesized and evaluated as antitumour and antimicrobial agents. The compounds that could be conveniently prepared in a few steps processes from natural safrole have been charac
Photoactivatable prodrugs of highly potent duocarmycin analogues for a selective cancer therapy
Tietze, Lutz F.,Müller, Michael,Duefert, Svenia-C.,Schmuck, Kianga,Schuberth, Ingrid
supporting information, p. 1726 - 1731 (2013/03/14)
A main problem of common cancer chemotherapy is the occurrence of severe side effects caused by insufficient selectivity of the applied drugs. A possible concept to overcome this limitation is light-driven prodrug monotherapy. The synthesis as well as photochemical and biological evaluation of new photoactivatable prodrugs is described. Best results were obtained with prodrug (S,S)-7 a. The photochemical labile protecting groups in (S,S)-7 a can easily be removed by irradiation with UV-A light in 30 min with a power of only 2 J cm-2. The determination of the in vitro cytotoxicity by using an HTCFA-test reveals a QIC50 value of 8200 and the prodrug is more than two million times less cytotoxic than the corresponding seco-drug (-)-(S,S)-5 with an IC50 value of about 110 fM. The big therapeutic window makes (S,S)-7 a very suitable for its use in selective cancer therapy. Copyright
Synthesis and antitumour evaluation of peptidyl-like derivatives containing the 1,3-benzodioxole system
Moreira, Diogo Rodrigo de Magalhaes,Lima Leite, Ana Cristina,Pinheiro Ferreira, Paulo Michel,da Costa, Patricia Marcal,Costa Lotufo, Leticia Veras,de Moraes, Manoel Odorico,Brondani, Dalci Jose,do O Pessoa, Claudia
, p. 351 - 357 (2007/10/03)
In the scope of a research program aiming at the synthesis and pharmacological evaluation of novel possible antitumour prototype compounds, we described in this paper the synthesis of peptidyl-like derivatives containing the 1,3-benzodioxole system. The proliferation inhibitors tested against tumour cell lines identified the derivatives tyrosine (4f) and lysine (4g) as the most active among them, presenting IC50 values in micromolar range and are more active than Safrole. For the study on the embryonic development, Safrole did not show any selectivity in this latter assay, which indicates that Safrole acts as a 'cell cycle-nonspecific' inhibitory agent. However, compound 4f presented a fair antimitotic effect, mainly on third cleavage and blastulae stages (38% and 1.7% of normal development, at 10 μg/mL), suggesting a time-dependent activity and a 'cell cycle-specific' agent action. Neither derivatives revealed hemolytic action in assay with mouse erythrocytes.
