- Improved, gram-scale synthesis of sildenafil in water using arylacetic acid as the acyl source in the pyrazolo[4,3-d]pyrimidin-7-one ring formation
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An improved, gram-scale synthesis of the blockbuster drug sildenafil, used for the treatment of male erectile dysfunction, has been developed. Unlike the previous literature, the current method demonstrates the use of arylacetic acid as an acyl source, a cheap oxidant K2S2O8, and water as the reaction medium in the key step of pyrrazolo[4,3-d]pyrimidin-7-one ring formation. As well as being a green and benign approach, the current method reduces the cost by half compared to our previous strategy. In addition, the general relevance of the method has been demonstrated in the synthesis of a variety of quinazolinone and benzothiazole derivatives with excellent functional group tolerance.
- Laha, Joydev K.,Gulati, Upma,Saima,Gupta, Anjali,Indurthi, Harish Kumar
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supporting information
p. 2643 - 2648
(2021/02/16)
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- Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents
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The first direct activator of BAX, a pro-apoptotic member of the BCL-2 family, has been recently identified. Herein, a structure-based lead optimization turned out into a small series of analogues, where 8 is the most potent compound published so far. 8 was used as pharmacological tool to ascertain, for the first time, the anticancer potential of BAX direct activators and the obtained results would suggest that BAX direct activators are potential future anticancer drugs rather than venoms.
- Brancaccio, Diego,Cassese, Hilde,Coluccia, Antonio,Di Maro, Salvatore,Giustiniano, Mariateresa,Grassia, Gianluca,Ialenti, Armando,La Pietra, Valeria,La Regina, Giuseppe,Marinelli, Luciana,Martini, Claudia,Novellino, Ettore,Passacantilli, Sara,Silvestri, Romano,Stornaiuolo, Mariano,Taliani, Sabrina
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p. 2135 - 2148
(2015/03/30)
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