A Cytostatic Ruthenium(II)–Platinum(II) Bis(terpyridyl) Anticancer Complex That Blocks Entry into S Phase by Up‐regulating p27^KIP1

Abstract

Article:Ramu, V., Gill, M.R., Jarman, P.J. et al. (4 more authors) (2015) A cytostatic ruthenium(II)-platinum(II) bis(terpyridyl) anticancer complex that blocks entry into S phase by up-regulating p27KIP1. Chemistry -A European Journal, 21 (25).

A ruthenium polypyridyl intercalator stalls DNA replication forks, radiosensitizes human cancer cells and is enhanced by Chk1 inhibition

“…Consistent with this, relatively low levels of the DSB-marker γH2AX (p-H2AX at Ser139)41 occur in lysates of cells treated with 1 (Figs 4a,b and S13). As expected842, substantial Chk2 phosphorylation and γH2AX expression was observed in cells treated with the DSB-generating agents MX or cisplatin. In comparison to the cellular response to 1 , treatment with 2 resulted in lower levels of phosphorylated DDR proteins, indicating a reduced DDR activation in cells exposed to the hydroxyl-substituted complex (Figs 4b and S13).…”

Two‐Photon‐Induced CO‐Releasing Molecules as Molecular Logic Systems in Solution, Polymers, and Cells

“…As anticipated from previous reports, the presence of long aliphatic chain in biotin structure could increase the overall lipophilicity of 2 when compared to nonbiotin conjugated 1 (Table ). The lipophilicity (log P ) values for both the photoCORMs were calculated using octanol/water shake flask method . It is not just noticeable that the biotin‐conjugate 2 shows higher uptake with brighter emission, but also reveals the characteristic feature of a biotin‐receptor‐mediated endocytosis in the form of additional clearly visible intracellular vesicle‐like particles (Figure c).…”

“…The lipophilicity (logP)v alues for both the photo-CORMsw ere calculated using octanol/water shake flask method. [46] It is not just noticeable that the biotin-conjugate 2 shows higher uptake with brighter emission, but also reveals the characteristic feature of ab iotin-receptor-mediated endocytosis in the form of additional clearly visible intracellular vesicle-like particles (Figure 2c). These observations suggest,t hat the enhanced uptake of 2 compared to its pendant 1 is not simply caused by higherl ipophilicity of biotin's aliphatic chain of compound 2 (Figure 2a).…”

Photo-induced cytotoxicity and anti-metastatic activity of ruthenium(ii)–polypyridyl complexes functionalized with tyrosine or tryptophan

“…Such changes are not uncommon for reagents that are not bound to DNA structure though intercalative mode of binding. 30,31 Luminescence studies revealed that addition of CT-DNA to the aq. buffer solutions of 1 and 2 led to the enhancement in the fluorescence intensity of the respective complexes.…”