Novel “ruthenium cyclopentadienyl”–peptide conjugate complexes against human FGFR(+) breast cancer

2020 ◽  
Vol 49 (18) ◽  
pp. 5974-5987
Author(s):  
João Franco Machado ◽  
Miguel Machuqueiro ◽  
Fernanda Marques ◽  
M. Paula Robalo ◽  
M. Fátima M. Piedade ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Biological Evaluation ◽  
Peptide Conjugates ◽  
Half Sandwich

Synthesis of the first half-sandwich ruthenium(ii)-cyclopentadienyl peptide conjugates and their biological evaluation against human FGFR(+) and FGFR(−) breast cancer cells.

scholarly journals Synthesis and Biological Evaluation of 1-(Diarylmethyl)-1H-1,2,4-triazoles and 1-(Diarylmethyl)-1H-imidazoles as a Novel Class of Anti-Mitotic Agent for Activity in Breast Cancer

2021 ◽  
Vol 14 (2) ◽  
pp. 169
Author(s):  
Gloria Ana ◽  
Patrick M. Kelly ◽  
Azizah M. Malebari ◽  
Sara Noorani ◽  
Seema M. Nathwani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Mitotic Catastrophe ◽  
Phase Cell ◽  
Computational Docking ◽  
Er Positive ◽  
Mcf 7

We report the synthesis and biochemical evaluation of compounds that are designed as hybrids of the microtubule targeting benzophenone phenstatin and the aromatase inhibitor letrozole. A preliminary screening in estrogen receptor (ER)-positive MCF-7 breast cancer cells identified 5-((2H-1,2,3-triazol-1-yl)(3,4,5-trimethoxyphenyl)methyl)-2-methoxyphenol 24 as a potent antiproliferative compound with an IC50 value of 52 nM in MCF-7 breast cancer cells (ER+/PR+) and 74 nM in triple-negative MDA-MB-231 breast cancer cells. The compounds demonstrated significant G2/M phase cell cycle arrest and induction of apoptosis in the MCF-7 cell line, inhibited tubulin polymerisation, and were selective for cancer cells when evaluated in non-tumorigenic MCF-10A breast cells. The immunofluorescence staining of MCF-7 cells confirmed that the compounds targeted tubulin and induced multinucleation, which is a recognised sign of mitotic catastrophe. Computational docking studies of compounds 19e, 21l, and 24 in the colchicine binding site of tubulin indicated potential binding conformations for the compounds. Compounds 19e and 21l were also shown to selectively inhibit aromatase. These compounds are promising candidates for development as antiproliferative, aromatase inhibitory, and microtubule-disrupting agents for breast cancer.

scholarly journals Synthesis and Characterisation of Novel Tricyclic and Tetracyclic Furoindoles: Biological Evaluation as SAHA Enhancer against Neuroblastoma and Breast Cancer Cells

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5745
Author(s):  
Murat Bingul ◽  
Greg M. Arndt ◽  
Glenn M. Marshall ◽  
David StC. Black ◽  
Belamy B. Cheung ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Histone Deacetylase Inhibitors ◽  
Methyl Esters ◽  
Biological Evaluation ◽  
Suberoylanilide Hydroxamic Acid ◽  
Ic50 Value ◽  
Anti Cancer ◽  
Cancer Activity

The dihydropyranoindole structures were previously identified as promising scaffolds for improving the anti-cancer activity of histone deacetylase inhibitors. This work describes the synthesis of related furoindoles and their ability to synergize with suberoylanilide hydroxamic acid (SAHA) against neuroblastoma and breast cancer cells. The nucleophilic substitution of hydroxyindole methyl esters with α-haloketones yielded the corresponding arylether ketones, which were subsequently cyclized to tricyclic and tetracyclic furoindoles. The furoindoles showed promising individual cytotoxic efficiency against breast cancer cells, as well as decent SAHA enhancement against cancer cells in select cases. Interestingly, the best IC50 value was obtained with the non-cyclized intermediate.

Steroidal N-Sulfonylimidates: Synthesis and biological evaluation in breast cancer cells

2019 ◽  
Vol 179 ◽  
pp. 694-706 ◽  
Author(s):  
Yulia A. Volkova ◽  
Andrey S. Kozlov ◽  
Marya K. Kolokolova ◽  
Denis Y. Uvarov ◽  
Sergey A. Gorbatov ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

New Thiophene Analogues of Kenpaullone: Synthesis and Biological Evaluation in Breast Cancer Cells.

ChemInform ◽  
2005 ◽  
Vol 36 (52) ◽  
Author(s):  
Laurent Brault ◽  
Evelyne Migianu ◽  
Adrien Neguesque ◽  
Eric Battaglia ◽  
Denyse Bagrel ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Half-sandwich Os(ii) and Ru(ii) bathophenanthroline complexes: anticancer drug candidates with unusual potency and a cellular activity profile in highly invasive triple-negative breast cancer cells

2018 ◽  
Vol 47 (35) ◽  
pp. 12197-12208 ◽  
Author(s):  
Jitka Pracharova ◽  
Vojtech Novohradsky ◽  
Hana Kostrhunova ◽  
Pavel Štarha ◽  
Zdeněk Trávníček ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Anticancer Drug ◽  
Triple Negative Breast Cancer ◽  
Breast Cancer Cells ◽  
Triple Negative ◽  
Cellular Activity ◽  
Activity Profile ◽  
Drug Candidates ◽  
Half Sandwich

A half-sandwich Os(ii) bathophenanthroline complex is a potent agent against highly progressive, poorly treatable triple-negative breast cancer cells.

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