Indoles as anticancer agents

Sayed, Mardia T. El; Hamdy, Nehal A.; Osman, Dalia Ahmed A.; Ahmed, Khadiga M.

doi:10.18282/amor.v1.i1.12

Cited by 52 publications

(28 citation statements)

References 105 publications

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“…28) As described in the Introduction part, a number of indole compounds have been shown to induce cell death such as apoptosis by numerous mechanisms. 4,5) Thus, the effects of MW-03 on cellular growth were evaluated in LS174T cells treated with 0.1 to 10 µM of MW-03 for 48 h. As shown in Fig. 3B, the treatments with MW-03 inhibited cellular growth in a concentration-dependent manner in LS174T cells.…”

Section: Effects Of Mw-03 On Pge 2 -Induced Camp Formationmentioning

confidence: 95%

“…4,5) These indole derivatives have been shown to induce cancer cell death such as apoptosis; although many mechanisms are suggested and reported, 4,5) the exact mechanisms underlying currently remain unclear. These cell death mechanisms are not only exerted by phytochemical indoles, but also by synthesized indoles such as one popular non-steroidal anti-inflammatory drug (NSAID), indomethacin.…”

Section: )mentioning

confidence: 99%

“…4,5) The consumption of cruciferous vegetables has been recommended by the National Research Council in the United States because of the protective mechanisms of phytochemicals including derivatives of indoles, e.g. indole-3-carbinol and diindolylmethane.4,5) These indole derivatives have been shown to induce cancer cell death such as apoptosis; although many mechanisms are suggested and reported, 4,5) the exact mechanisms underlying currently remain unclear. These cell death mechanisms are not only exerted by phytochemical indoles, but also by synthesized indoles such as one popular non-steroidal anti-inflammatory drug (NSAID), indomethacin.…”

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confidence: 99%

“…3) Cruciferous vegetables, such as cauliflower, cabbage, and broccoli, are regarded as good food sources for reducing the risk of cancer including colon cancer. 4,5) Natural compounds that contain indole structures are relatively rich in cruciferous vegetables. 4,5) The consumption of cruciferous vegetables has been recommended by the National Research Council in the United States because of the protective mechanisms of phytochemicals including derivatives of indoles, e.g.…”

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confidence: 99%

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Anti-cancer Effects of MW-03, a Novel Indole Compound, by Inducing 15-Hydroxyprostaglandin Dehydrogenase and Cellular Growth Inhibition in the LS174T Human Colon Cancer Cell Line

Seira

Yanagisawa

Suganami

et al. 2017

Biological & Pharmaceutical Bulletin

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Increases in the expression of prostaglandin E 2 (PGE 2 ) are widely known to be involved in aberrant growth in the early stage of colon cancer development. We herein demonstrated that the novel indole compound MW-03 reduced PGE 2 -induced cAMP formation by catalization to an inactive metabolite by inducing 15-hydroxyprostaglandin dehydrogenase through the activation of peroxisome proliferator-activated receptor-γ. MW-03 also inhibited colon cancer cell growth by arresting the cell cycle at the S phase. Although the target of MW-03 for cell cycle inhibition has not yet been identified, these dual anti-cancer effects of MW-03 itself and/or its leading compound(s) on colon cancer cells may reduce colon cancer development and, thus, have potential as a novel treatment for the early stage of this disease.Key words indole compound; MW-03; prostaglandin E 2 ; 15-hydroxyprostaglandin dehydrogenase; peroxisome proliferator-activated receptor-γ; colon cancer One major prostanoid, prostaglandin E 2 (PGE 2 ) is widely known to be up-regulated by the action of increased levels of cyclooxygenase-2 (COX-2) in colorectal cancer.1,2) Thus, the enhanced expression of COX-2 and biosynthesis of PGE 2 are responsible for the malignancy of diseases.1,2) Since the overexpression of COX-2 and PGE 2 is frequently observed in the early stage of colorectal cancer development, they are considered to be the biomarkers of this stage. 3)Cruciferous vegetables, such as cauliflower, cabbage, and broccoli, are regarded as good food sources for reducing the risk of cancer including colon cancer. 4,5) Natural compounds that contain indole structures are relatively rich in cruciferous vegetables. 4,5) The consumption of cruciferous vegetables has been recommended by the National Research Council in the United States because of the protective mechanisms of phytochemicals including derivatives of indoles, e.g. indole-3-carbinol and diindolylmethane.4,5) These indole derivatives have been shown to induce cancer cell death such as apoptosis; although many mechanisms are suggested and reported, 4,5) the exact mechanisms underlying currently remain unclear. These cell death mechanisms are not only exerted by phytochemical indoles, but also by synthesized indoles such as one popular non-steroidal anti-inflammatory drug (NSAID), indomethacin. 6,7)Some indole compounds have been used as tools for researching prostanoid receptors and/or their signaling pathways. Among them, indomethacin has been used as an E-type prostanoid 2 (EP2) prostanoid receptor antagonist, 8) D-type prostanoid receptor antagonist, 9,10) chemoattractant receptorhomologous molecule expressed on T helper 2 cell receptor agonist, 11) and peroxisome proliferator-activated receptor-γ (PPARγ) agonist/antagonist, 12,13) by itself and/or its leading compounds with cyclooxygenase inhibition-independent activities.14) A previous study reported that indomethacin induced 15-hydroxyprostaglandin dehydrogenase (15-PGDH), an enzyme that catalyzes prostanoids such as PGE 2 to inactive, the metabolite...

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Section: Effects Of Mw-03 On Pge 2 -Induced Camp Formationmentioning

confidence: 95%

Section: )mentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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Anti-cancer Effects of MW-03, a Novel Indole Compound, by Inducing 15-Hydroxyprostaglandin Dehydrogenase and Cellular Growth Inhibition in the LS174T Human Colon Cancer Cell Line

Seira

Yanagisawa

Suganami

et al. 2017

Biological & Pharmaceutical Bulletin

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“…The indole derivatives are known to possess anticancer, antioxidant, antitumor, and anti-HIV [8][9][10][11]28] activities.…”

Section: Introductionmentioning

confidence: 99%

Design and Synthesis of Benzodiazepines Bearing Benzimidazole/Benzothiazole and Indole Moieties as a Potent Antimicrobial and Antioxidant Agents

Naraboli

Biradar

2018

Asian J Pharm Clin Res

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Objective: The present work deals with the synthesis and characterization of biologically active new indole derivatives, namely, 2-Methods: All these newly synthesized compounds were screened for their in vitro antimicrobial activity by an agar plate diffusion method, antioxidant activities such as 1,1-diphenyl-2-picrylhydrazyl (DPPH), radical scavenging activity (RSA), ferric ions (Fe Result:The structures of all the newly synthesized compounds were characterized by their infrared, 1 H nuclear magnetic resonance, mass spectral studies, and elemental analysis. Compounds 7a and 7b exhibited good RSA at a concentration 100 µg/ml, compounds 6d, 7a-d and 8a-c displayed good FRAP at a concentration 100 µg/ml, compounds 7b-d and 8b-d showed good Fe 2+ ion metal chelating activity. Compounds 6b, 6d, 7a-d, and 8a-d exhibited good activity against all the screened bacteria and fungi.Conclusion: Some of the compounds have shown potent antimicrobial activity against all the screened bacteria and fungi, and some have exhibited very good antioxidant activity.

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Cascade Synthesis of New Indole‐Containing Pentacyclic Scaffolds Mediated by Aryl and Iminyl Radicals

Abonia,

García,

Hurtado

et al. 2024

Chemistry An Asian Journal

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A five‐step approach, starting from simple 1,5‐disubstituted indoles, has been implemented for the synthesis of diversely substituted indole‐pyrido‐indene pentacyclic compounds up to 54% yield via domino radical‐mediated processes in the presence of the radical reagents DLP/TTMSS and AIBN/TTMSS. Reactions proceeded with diverse key starting radical cyano‐precursors strategically synthesized which were subsequently transformed into the target pentacyclic compounds through an aryl/iminyl radical‐mediated domino reactions sequence. In addition to the routine spectroscopic techniques, the structure of radical precursors, as well as, the target pentacyclic products were unequivocally established by single crystal X‐ray diffraction, confirming the effectiveness of the proposed synthetic sequence.

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Indoles as anticancer agents

Cited by 52 publications

References 105 publications

Anti-cancer Effects of MW-03, a Novel Indole Compound, by Inducing 15-Hydroxyprostaglandin Dehydrogenase and Cellular Growth Inhibition in the LS174T Human Colon Cancer Cell Line

Anti-cancer Effects of MW-03, a Novel Indole Compound, by Inducing 15-Hydroxyprostaglandin Dehydrogenase and Cellular Growth Inhibition in the LS174T Human Colon Cancer Cell Line

Design and Synthesis of Benzodiazepines Bearing Benzimidazole/Benzothiazole and Indole Moieties as a Potent Antimicrobial and Antioxidant Agents

Cascade Synthesis of New Indole‐Containing Pentacyclic Scaffolds Mediated by Aryl and Iminyl Radicals

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