Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

The targeted approach of protein kinases (PKs), as PKs are the main regulators cell survival and proliferation, has been a promising strategy for cancer treatments. Here we analyse potential quinoline-carboxamide derivatives four lines: MCF-7, CACO, HepG-2 HCT-116 anticancer agents. 3e, 4b, 11b 13d showed good anti-proliferative activities in comparison to reference standard Doxorubicin, against lines tested. They have chosen further studies. First all, IC50 value surveys were carried out ensure protection our hits demonstrate that cytotoxic effect (IC50 > 113 μM) is highly selective on normal human cells (WI-38). Secondly, apoptosis was accomplished by down-regulation Bcl-2 up-regulation BAX Caspase-3 these active compounds. Also, Pim-1 inhibitory activity hybrids done, which indicates compound 3e most with percentage inhibition 82.27% equals 0.11 when compared SGI-1776 standard. In addition, silico assessment ADME properties, all strongest compounds orally bioavailable without blood–brain barrier penetration.