Correction: Griffith, D.M., et al. Novel Improved Synthesis of HSP70 Inhibitor, Pifithrin-μ. In Vitro Synergy Quantification of Pifithrin-μ Combined with Pt Drugs in Prostate and Colorectal Cancer Cells. Molecules 2016, 21, 949

McKeon, Aoife M; Egan, Alan; Chandanshive, Jay Zumbar; McMahon, Helena; Griffith, Darren M.

doi:10.3390/molecules21111550

Cited by 2 publications

(1 citation statement)

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“…We are interested in the functionalisation of Pt based complexes [19,20] and more recently in the development of click-based conjugation strategies [21,22]. The Cu(I) catalysed azide-alkyne cycloaddition (CuAAC), Fig.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterisation and in vitro antitumour potential of novel Pt(II) estrogen linked complexes

Kitteringham

Andriollo

Gandin

et al. 2019

Inorganica Chimica Acta

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The Cu(I) alkyne azide click reaction of 17α-ethynylestradiol and di-tert-butyl (2-azidopropane-1,3-diyl)dicarbamate afforded the novel 1,4 disubstituted 1,2,3 triazole and estrogen-based ligand 2-(4-(estradiol)-1H-1,2,3-triazol-1-yl)propane-1,3-diamine, EDiolDap. Reaction of EDiolDap with Pt(II) DMSO precursors, cis-[PtCl 2 (DMSO) 2 ] and cis-[Pt(CBDCA)(DMSO) 2 ] gave the corresponding Pt(II) estrogen linked complexes [PtCl 2 (EDiolDap)] and [Pt(CBDCA)(EDiolDap)] respectively in good yield. Both Pt(II) estrogen linked complexes exhibited superior activity as compared to cisplatin and carboplatin in 2D culture and exhibited ca. 30 fold higher activity, in terms of IC 50 values, against ER+ cancer cells (cervical, breast and ovarian) as compared to the reference ER− colon cancer line. [PtCl 2 (EDiolDap)] and [Pt(CBDCA)(EDiolDap)] retained their anti-tumour activity in an ovarian 3D spheroid culture model and reduced the viability of ovarian cancer cell spheroids ca. 9fold and 5-fold better, respectively, as compared to cisplatin.

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Section: Introductionmentioning

confidence: 99%

Synthesis, characterisation and in vitro antitumour potential of novel Pt(II) estrogen linked complexes

Kitteringham

Andriollo

Gandin

et al. 2019

Inorganica Chimica Acta

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Synthetic Small Molecule Modulators of Hsp70 and Hsp40 Chaperones as Promising Anticancer Agents

Nitzsche

Höpfner

Biersack

2023

IJMS

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A class of chaperones dubbed heat shock protein 70 (Hsp70) possesses high relevance in cancer diseases due to its cooperative activity with the well-established anticancer target Hsp90. However, Hsp70 is closely connected with a smaller heat shock protein, Hsp40, forming a formidable Hsp70-Hsp40 axis in various cancers, which serves as a suitable target for anticancer drug design. This review summarizes the current state and the recent developments in the field of (semi-)synthetic small molecule inhibitors directed against Hsp70 and Hsp40. The medicinal chemistry and anticancer potential of pertinent inhibitors are discussed. Since Hsp90 inhibitors have entered clinical trials but have exhibited severe adverse effects and drug resistance formation, potent Hsp70 and Hsp40 inhibitors may play a significant role in overcoming the drawbacks of Hsp90 inhibitors and other approved anticancer drugs.

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Correction: Griffith, D.M., et al. Novel Improved Synthesis of HSP70 Inhibitor, Pifithrin-μ. In Vitro Synergy Quantification of Pifithrin-μ Combined with Pt Drugs in Prostate and Colorectal Cancer Cells. Molecules 2016, 21, 949

Abstract: n/a

Cited by 2 publications

References 1 publication

Synthesis, characterisation and in vitro antitumour potential of novel Pt(II) estrogen linked complexes

Synthesis, characterisation and in vitro antitumour potential of novel Pt(II) estrogen linked complexes

Synthetic Small Molecule Modulators of Hsp70 and Hsp40 Chaperones as Promising Anticancer Agents

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