TY - JOUR
T1 - 7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors
AU - Cincinelli, Raffaella
AU - Musso, Loana
AU - Merlini, Lucio
AU - Giannini, Giuseppe
AU - Vesci, Loredana
AU - Milazzo, Ferdinando M.
AU - Carenini, Nives
AU - Perego, Paola
AU - Penco, Sergio
AU - Artali, Roberto
AU - Zunino, Franco
AU - Pisano, Claudio
AU - Dallavalle, Sabrina
PY - 2014/2/1
Y1 - 2014/2/1
N2 - 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
AB - 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
KW - 7-Azaindoles
KW - Antitumor
KW - Molecular modelling
KW - PARP inhibitors
KW - Synthesis
UR - http://www.scopus.com/inward/record.url?scp=84892805503&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84892805503&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2013.12.031
DO - 10.1016/j.bmc.2013.12.031
M3 - Article
C2 - 24398383
AN - SCOPUS:84892805503
VL - 22
SP - 1089
EP - 1103
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 3
ER -