Synthesis and biological evaluation of novel hydrazide based cytotoxic agents.
作者： Fedora Grande , Roppei Yamada , Xuefei Cao , Francesca Aiello , Antonio Garofalo
DOI: 10.1517/13543780902858815
关键词:
摘要: Recently, we designed and synthesized a series of pyrroloquinoxaline compounds with hydrazine moiety linking nitrogen-containing polycyclic group to heteroaroyl system. Several derivatives, attractive drug-like properties, were identified as promising cytotoxic agents, showing excellent potency in panel cancer cell lines. In the current study, further 19 new analogues optimize their physicochemical properties assess coherent mechanism action. chemical modifications made reference by varying fused-ring system and/or heteroacyl moiety. To evaluate vitro activity, tested these six human lines derived from different origins. Among them, two ( ) showed similar IC50 values sub-micromolar range all tested. Furthermore, compound vivo efficacy our preliminary ovarian mouse xenograft studie...
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