ArticleEuropean journal of medicinal chemistry2010
In vitro and in vivo studies on stilbene analogs as potential treatment agents for colon cancer.
Article in European journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 57 citations in OpenAlex.
- Detection of Biomedically Relevant Stilbenes from Wines by Mass Spectrometry: An Update.Advances in experimental medicine and biology · 2026Review
- Pinostilbene as a Potential Cytotoxic Agent in Cancer Cell Lines: Improvement of Solubility and Stability by Cyclodextrin Encapsulation.Pharmaceutics · 2025Article
- Polyphenols: From Classification to Therapeutic Potential and Bioavailability.Foods (Basel, Switzerland) · 2024Review
- Synthesis and antimicrobial activity of aminoalkyl resveratrol derivatives inspired by cationic peptides.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- HACS omega · 2023Article
- Cis-trimethoxystilbene, exhibits higher genotoxic and antiproliferative effects than its isomer trans-trimethoxystilbene in MCF-7 and MCF-10A cell lines.Genetics and molecular biology · 2021Article
- Synthetic approaches toward stilbenes and their related structures.Molecular diversity · 2017Review
- Comparative Depigmentation Effects of Resveratrol and Its Two Methyl Analogues in α-Melanocyte Stimulating Hormone-Triggered B16/F10 Murine Melanoma Cells.Preventive nutrition and food science · 2016Article
- Cancer prevention and therapy through the modulation of the tumor microenvironment.Seminars in cancer biology · 2015Review
- 3,4',5-trans-Trimethoxystilbene; a natural analogue of resveratrol with enhanced anticancer potency.Investigational new drugs · 2015Article
- A facile, stereoselective, one-pot synthesis of resveratrol derivatives.Chemistry Central journal · 2015Article
- 2',6'-Dihalostyrylanilines, pyridines, and pyrimidines for the inhibition of the catalytic subunit of methionine S-adenosyltransferase-2.Journal of medicinal chemistry · 2014Article
- Prevention and Treatment of Colorectal Cancer by Natural Agents From Mother Nature.Current colorectal cancer reports · 2013Article
- Resveratrol enhances antitumor activity of TRAIL in prostate cancer xenografts through activation of FOXO transcription factor.PloS one · 2010Article
- Synthesis and biological evaluation of retinoid-chalcones as inhibitors of colon cancer cell growth.Bioorganic & medicinal chemistry letters · 2010Article
- Cytotoxicity and genotoxicity of stilbene derivatives in CHO-K1 and HepG2 cell lines.Genetics and molecular biologyArticle
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
Based on the potential of resveratrol as a colon cancer chemopreventive agent, a set of 26 stilbenes were synthesized and tested against the colon cancer cell lines HT-29 and Caco-2. (Z)-4-(3,5-Dimethoxystyryl)aniline (4), (Z)-methyl-4-(3,5-dimethoxystyryl)benzoate (6), and (Z)-1,3-dimethoxy-5-(4-methoxystyryl)benzene (10) showed strong inhibitory activity in vitro. In vivo studies using HT-29 xenografts in immunodeficient mice were conducted with 4, 6 and 10, together with their corresponding trans isomers (3, 5, and 9, respectively), at the dose of 10 mg/kg body weight. Tumor volume was significantly lowered in 3-, 4-, and 9-treated groups. The cis- and trans-amino analogs (4 and 3, respectively) had similar effect on tumor growth, a 40% decrease compared to the control. Analysis of the serum revealed that 4 isomerized to 3, which may explain their similar effects in SCID mice. Stilbenes 5, 6, 9, and 10 retained their configurations in the serum. Stilbenes 6 and 10 lacked tumor-suppressive effect in SCID mice; the serum levels of these analogs were low (18.8 and 15.5 ng/mL, respectively). Stilbene 9, while weakly active in vitro demonstrated good activity in vivo, was found at higher levels in the serum (69.9 ng/mL) compared to 10. The anti-tumorigenic activity of these stilbene analogs may be partly linked to their effects on proteins involved in cell proliferation, as observed by lowered expression of proliferating cell nuclear antigen and upregulation of the cyclin-dependent kinase inhibitor, p27, in the tumor tissues. Overall, identification of the anti-tumorigenic potential of these compounds provides opportunities for their use against colorectal cancer.
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Registered trials
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