7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors.
Basic Information
ID: ALA3102753
Journal: Bioorg Med Chem
Title: 7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors.
Authors: Cincinelli R, Musso L, Merlini L, Giannini G, Vesci L, Milazzo FM, Carenini N, Perego P, Penco S, Artali R, Zunino F, Pisano C, Dallavalle S.
Abstract: 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.
CiteXplore: 24398383
DOI: 10.1016/j.bmc.2013.12.031
Patent ID: ┄