Solomon, V. Raja; Pundir, Sheetal; Lee, Hoyun published the article 《Examination of novel 4-aminoquinoline derivatives designed and synthesized by a hybrid pharmacophore approach to enhance their anticancer activities》. Keywords: structure activity aminoquinoline antitumor; bortezomib monastrol aminoquinoline derivative anticancer breast cancer progression.They researched the compound: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5 ).Category: bromides-buliding-blocks. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:837-52-5) here.
In an attempt to develop effective and potentially safe anticancer agents, thirty-six 4-aminoquinoline-derived sulfonyl analogs I (R = CH3, 4-ClC6H4, p-tolyl, etc., X = Cl, CF3) and II were designed and synthesized using a hybrid pharmacophore approach. The cytotoxicity of these compounds was determined using three breast tumor cell lines (MDA-MB231, MDA-MB468 and MCF7) and two matching non-cancer breast epithelial cell lines (184B5 and MCF10A). Although most of the compounds were quite effective on the breast cancer cells, I [R = 2,4-(O2N)2C6H3, X = Cl] (III; VR23) emerged as potentially the most desirable one in this series of compounds Data from the NCI-60 cancer panel screening show that compound III is effective on a wide range of different cancers. Importantly, compound III needed up to 17.6-fold less doses to achieve the same IC50 against cancer than non-cancer cells (MDA-MB468 vs MCF10A), suggesting that it can potentially be less toxic to normal cells. Cancer cells formed multiple centrosomes in the presence of compound III, resulting in the cell cycle arrest at prometa-meta phase. This abnormality leads to eventual cell demise with sub-G1 DNA content typically shown with apoptotic cells. In addition, compound III also causes an increase in lysosomal volume in cancer but not in non-cancer cells, which may contribute at least in part to its preferential cancer cell-killing. The cancer cell-killing effect of compound III is highly potentiated when combined with either bortezomib or monastrol.
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Reference:
Bromide – Wikipedia,
bromide – Wiktionary