Novel HDAC6 selective inhibitors with 4-aminopiperidine-1- carboxamide as the core structure enhanced growth inhibitory activity of bortezomib in MCF-7 cells

Cationic nanovectors loaded with Ru-based nucleolipids exert a high growth-inhibitory activity against human cancer cells (MCF-7 (A), WiDr (B), and HeLa (C)).

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Troglitazone enhances tamoxifen-induced growth inhibitory activity of MCF-7 cells

Biochemical and Biophysical Research Communications ◽

10.1016/j.bbrc.2008.09.111 ◽

2008 ◽

Vol 377 (1) ◽

pp. 242-247 ◽

Cited By ~ 15

Author(s):

Hong-Nu Yu ◽

Eun-Mi Noh ◽

Young-Rae Lee ◽

Si-Gyun Roh ◽

Eun-Kyung Song ◽

...

Keyword(s):

Inhibitory Activity ◽

Growth Inhibitory ◽

Growth Inhibitory Activity ◽

Mcf 7

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New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential

Future Medicinal Chemistry ◽

10.4155/fmc-2018-0285 ◽

2019 ◽

Vol 11 (13) ◽

pp. 1583-1603

Author(s):

Ashraf M Omar ◽

Heba A Abd El Razik ◽

Aly A Hazzaa ◽

Maryam AZ El-Attar ◽

Maha A El Demellawy ◽

...

Keyword(s):

Free Radicals ◽

Inhibitory Activity ◽

Docking Studies ◽

Cyclooxygenase 1 ◽

Growth Inhibitory ◽

Growth Inhibitory Activity ◽

Cox 2 ◽

Inhibitory Potential ◽

Cox 1 ◽

Mcf 7

Aim: Cyclooxygenase-2 (COX-2) inhibition and scavenging-free radicals are important targets in cancer treatment. Materials & methods: Sulfanylpyrimidines and triazolopyrimidines were synthesized and evaluated as anticancer and antioxidant COX-1/2 inhibitors. Results: Compound 7 showed the same growth inhibitory activity as 5-fluorouracil against MCF-7. Compound 6f displayed broad-spectrum anticancer activity against the four tested cancer cell lines. Compounds 5b, 6a, 6c, 6d and 8 were found to be more active antioxidants than trolox. Compounds 6a, 6c, 6f and 8 revealed high COX-2 inhibitory activity and selectivity, which was confirmed by docking studies. Conclusion: Compound 6f could be considered as promising anticancer and antioxidant structural lead with COX-2 inhibition that deserve further derivatization and investigation.

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A New Triterpenoid Alkaloid from Buxus sempervirens

Zeitschrift für Naturforschung B ◽

10.1515/znb-2011-1013 ◽

2011 ◽

Vol 66 (10) ◽

pp. 1076-1078 ◽

Cited By ~ 1

Author(s):

Yu-Xin Yan ◽

Yun Sun ◽

Jian-Chao Chen ◽

Jia Su ◽

Yan Li ◽

...

Keyword(s):

Cytotoxic Activity ◽

Spectral Data ◽

Human Cell ◽

Spectral Methods ◽

Inhibitory Activity ◽

Human Cell Lines ◽

Growth Inhibitory ◽

Growth Inhibitory Activity ◽

Buxus Sempervirens ◽

Mcf 7

A new triterpenoid alkaloid, 16-deacetoxy-hyrcamine (1), together with six analogs, was isolated from the leaves and stems of Buxus sempervirens. Their structures were elucidated based on spectral methods and by comparison of the spectral data with those reported previously. All isolated compounds were evaluated for their growth inhibitory activity against human cell lines HL-60, SMMC-7721, A-549,MCF-7, and SW480. Compounds 1 - 4 and 6 showed modest cytotoxic activity against A-549, MCF-7, and SW480.

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Modifications on the Tetrahydroquinoline Scaffold Targeting a Phenylalanine Cluster on GPER as Antiproliferative Compounds against Renal, Liver and Pancreatic Cancer Cells

Pharmaceuticals ◽

10.3390/ph14010049 ◽

2021 ◽

Vol 14 (1) ◽

pp. 49

Author(s):

David Méndez-Luna ◽

Loreley Araceli Morelos-Garnica ◽

Juan Benjamín García-Vázquez ◽

Martiniano Bello ◽

Itzia Irene Padilla-Martínez ◽

...

Keyword(s):

Binding Site ◽

Cell Lines ◽

Cancer Cell ◽

Inhibitory Activity ◽

In Silico ◽

Cancer Cell Lines ◽

Pancreatic Cancer Cells ◽

Growth Inhibitory ◽

Growth Inhibitory Activity ◽

New Compounds

The implementation of chemo- and bioinformatics tools is a crucial step in the design of structure-based drugs, enabling the identification of more specific and effective molecules against cancer without side effects. In this study, three new compounds were designed and synthesized with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-tox) properties and high affinity for the G protein-coupled estrogen receptor (GPER) binding site by in silico methods, which correlated with the growth inhibitory activity tested in a cluster of cancer cell lines. Docking and molecular dynamics (MD) simulations accompanied by a molecular mechanics/generalized Born surface area (MMGBSA) approach yielded the binding modes and energetic features of the proposed compounds on GPER. These in silico studies showed that the compounds reached the GPER binding site, establishing interactions with a phenylalanine cluster (F206, F208 and F278) required for GPER molecular recognition of its agonist and antagonist ligands. Finally, a 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide (MTT) assay showed growth inhibitory activity of compounds 4, 5 and 7 in three different cancer cell lines—MIA Paca-2, RCC4-VA and Hep G2—at micromolar concentrations. These new molecules with specific chemical modifications of the GPER pharmacophore open up the possibility of generating new compounds capable of reaching the GPER binding site with potential growth inhibitory activities against nonconventional GPER cell models.

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Indole-3-carbinol inhibits the proliferation of colorectal carcinoma LoVo cells through activation of the apoptotic signaling pathway

Human & Experimental Toxicology ◽

10.1177/09603271211021475 ◽

2021 ◽

pp. 096032712110214

Author(s):

JY Lee ◽

HM Lim ◽

CM Lee ◽

S-H Park ◽

MJ Nam

Keyword(s):

Colorectal Carcinoma ◽

Cancer Cells ◽

Inhibitory Activity ◽

Annexin V ◽

Fluorescein Isothiocyanate ◽

Cell Counting ◽

Terminal Deoxynucleotidyl Transferase ◽

Growth Inhibitory ◽

Growth Inhibitory Activity ◽

Lovo Cells

Indole-3-carbinol (I3C) is a phytochemical that exhibits growth-inhibitory activity against various cancer cells. However, there are limited studies on the effects of I3C on colon cancer cells. In this study, the growth-inhibitory activity of I3C against the human colorectal carcinoma cell line (LoVo) was examined. The results of the 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide, colony formation, and cell counting assays revealed that I3C suppressed the proliferation of LoVo cells. Microscopy and wound-healing analyses revealed that I3C affected the morphology and inhibited the migration of LoVo cells, respectively. I3C induced apoptosis and DNA fragmentation as evidenced by the results of fluorescein isothiocyanate-conjugated annexin V staining and terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick-end labeling assay, respectively. Additionally, I3C arrested the cell cycle at the G0/G1 phase and enhanced the reactive oxygen species levels. Western blotting analysis revealed that treatment with I3C resulted in the activation of apoptotic proteins, such as poly(ADP-ribose) polymerase, caspase-3, caspase-7, caspase-9, Bax, Bim, and p53 in LoVo cells. These results indicate that I3C induces apoptosis in LoVo cells by upregulating p53, leading to the activation of Bax and caspases. Taken together, I3C exerts cytotoxic effects on LoVo cells by activating apoptosis.

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