PMID: 20126988Feb 4, 2010Paper

Bioactivity and molecular targets of novel substituted quinolines in murine and human tumor cell lines in vitro

International Journal of Oncology
Elisabeth M PerchelletJean-Pierre H Perchellet

Abstract

Substituted quinolines (PQ code number), which reduce colony formation and increase gap junctional intercellular communication, were tested for their ability to interact with various molecular targets in murine and human tumor cell lines in vitro. Various markers of tumor cell metabolism, DNA fragmentation, mitotic disruption, apoptosis induction and growth factor receptor signaling pathways were assayed in vitro to evaluate drug cytotoxicity. Based on its ability to inhibit the metabolic activity of suspension cultures of leukemic L1210 cells at days 2 and 4 in vitro, PQ1 succinic acid salt is the most effective antiproliferative agent among the synthetic quinoline analogs tested. Moreover, antiproliferative PQ1 is effective across a spectrum of monolayer cultures of pancreatic Pan02, epidermoid A-431 and mammary SK-BR-3 and BT-474 tumor cells. PQ1 also blocks Ki-67 expression, a marker of tumor cell proliferation. A 1.5- to 3-h treatment with PQ1 is sufficient to inhibit the incorporations of [3H]-thymidine into DNA, [3H]-uridine into RNA and [3H]-leucine into protein used to assess the rates of macromolecule syntheses over a 0.5- or 1-h period of pulse-labeling in L1210 tumor cells. A 15-min pretreatment with PQ1 inhibits th...Continue Reading

Citations

Jun 11, 2015·Future Medicinal Chemistry·Po-Yee ChungKim-Hung Lam
Feb 17, 2015·Cancer Cell International·Michael JelínekJan Kovář
Nov 18, 2020·Archives of Medical Research·Baris ErtugrulBedia Cakmakoglu

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