1542067-01-5Relevant academic research and scientific papers
7-AZAINDOLE DERIVATIVES AS PARP INHIBITORS
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Page/Page column 12; 13, (2015/02/19)
The present invention relates to 7-azaindole derivatives of Formula (I), pharmaceutical compositions containing such derivatives. The invention further relates to said pharmaceutical compositions for use in medicine, and more particularly in the treatment of cancer diseases where an inhibition of PARP is responsive.
7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors
Cincinelli, Raffaella,Musso, Loana,Merlini, Lucio,Giannini, Giuseppe,Vesci, Loredana,Milazzo, Ferdinando M.,Carenini, Nives,Perego, Paola,Penco, Sergio,Artali, Roberto,Zunino, Franco,Pisano, Claudio,Dallavalle, Sabrina
, p. 1089 - 1103 (2014/02/14)
7-Azaindole-1-carboxamides were designed as a new class of PARP-1 inhibitors The compounds displayed a variable pattern of target inhibition profile that, in part, paralleled the antiproliferative activity in cell lines characterized by homologous recombination defects A selected compound (1l; ST7710AA1) showed significant in vitro target inhibition and capability to substantially bypass the multidrug resistance mediated by Pgp In antitumor activity studies against the MX1 human breast carcinoma growth in nude mice, the compound exhibited an effect similar to that of Olaparib in terms of tumor volume inhibition when used at a lower dose than the reference compound Treatment was well tolerated, as no deaths or significant weight losses were observed among the treated animals
