A computational study to explore the molecular mechanisms behind the antiproliferative activity of Nortopsentin derivatives

2018

A facile synthesis of 1-ethyl-3-methyl-11-phenyl-1,4-dihydro-5H-pyrazolo[3,4-c][1,5]benzodiazocin-5-ones. A new ring system

2007

The new ring system pyrazolo[3,4-c][1,5]benzodiazocine was obtained through cyclization of the key intermediate of type 6a-d and 9, in refluxing toluene in presence of a catalytic amount of p-toluensulfonic acid, from moderate to high yields

PRC2 allosteric modulation an alternative strategy in drug discovery for the epigenetic diseases

2018

Role of hypoxia in pemetrexed-resistance of mesothelioma mediated by proton-coupled folate transporter, and preclinical activity of new anti-LDH comp…

2018

Introduction There are few effective therapies for malignant pleural mesothelioma (MPM), which remains one of the most lethal cancers. We previously demonstrated that low expression of the PCFT transporter, both at mRNA and protein levels, is associated with shorter survival of MPM patients treated with pemetrexed (Giovannetti et al., 2017). Since hypoxia has also been associated to antifolate-resistance (Raz et al, 2014), this study was aimed at elucidating key factors in pemetrexed resistance and hypoxia that may contribute to the rational development of novel therapeutic interventions against mesothelioma. Methods The levels of PCFT and of the hypoxia marker carbonic anhydrase-IX were de…

Synthesis and antiproliferative activity of [1,2,4] triazino[4,3-a]indoles

2005

A series of [1, 2, 4triazino[4,3-a]indoles was prepared in good yield by reacting 2-diazo-3-ethoxycarbonylindole with methylene active compounds. Derivatives of the title ring system were tested against a panel of 60 human tumor cell lines, and showed inhibitory activity against a wide range of cancer cell lines at micromolar concentration.