quercetin and Colonic-Neoplasms

quercetin has been researched along with Colonic-Neoplasms* in 4 studies

Other Studies

4 other study(ies) available for quercetin and Colonic-Neoplasms

ArticleYear
Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases.
    Bioorganic & medicinal chemistry letters, 2012, Jan-15, Volume: 22, Issue:2

    The alpha isoform of the phosphatidylinositol-3-kinases (PI3Kα) is often mutated, amplified and overexpressed in human tumors. In an effort to develop new inhibitors targeting this enzyme, we carried out a pharmacophore model study based on six PI3Kα-selective compounds. The pharmacophore searching identified three structurally novel inhibitors of PI3Kα and its H1047R mutant. Our biological studies show that two of our hit molecules suppressed the formation of pAKT, a downstream effector of PI3Kα, and induced apoptosis in the HCT116 colon cancer cell line. QPLD-based docking showed that residues Asp933, Glu849, Val851, and Gln859 appeared to be key binding residues for active inhibitors.

    Topics: Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Colonic Neoplasms; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Structure; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Protein Kinase Inhibitors; Stereoisomerism; Structure-Activity Relationship

2012
Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: an SAR study.
    Journal of medicinal chemistry, 2005, Apr-21, Volume: 48, Issue:8

    A library of 42 natural and synthetic flavonoids has been screened for their effect on cell proliferation and apoptosis in a human colonic cell line (HT-29). Examples of different classes of flavonoids have been screened, and the effects of hydroxylation, methoxylation and/or C-alkylation at various positions in the A- and B-rings have been assessed. Flavones and flavonols possess greater antiproliferative activity than chalcones and flavanones. With respect to structural modification of flavonoids, C-isoprenylation was by far the most effective, with substitution at the 8-position and longer chains, such as geranyl giving the best results. Finally, most compounds that significantly reduced cell survival also increased caspase activity, suggesting that at least part of their antiproliferative activity might be attributable to an apoptotic response.

    Topics: Alkylation; Antineoplastic Agents; Apoptosis; Caspases; Cell Line, Tumor; Cell Proliferation; Chalcone; Colonic Neoplasms; Enzyme Activators; Flavones; Flavonoids; Humans; Hydroxylation; Structure-Activity Relationship

2005
New bioactive polyphenols from Theobroma grandiflorum ("cupuaçu").
    Journal of natural products, 2003, Volume: 66, Issue:11

    Activity-guided fractionation of Theobroma grandiflorum ("cupuaçu") seeds resulted in the identification of two new sulfated flavonoid glycosides, theograndins I (1) and II (2). In addition, nine known flavonoid antioxidants, (+)-catechin, (-)-epicatechin, isoscutellarein 8-O-beta-d-glucuronide, hypolaetin 8-O-beta-d-glucuronide, quercetin 3-O-beta-d-glucuronide, quercetin 3-O-beta-d-glucuronide 6' '-methyl ester, quercetin, kaempferol, and isoscutellarein 8-O-beta-d-glucuronide 6' '-methyl ester, were identified. Theograndin II (2) displayed antioxidant activity (IC(50) = 120.2 microM) in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free-radical assay, as well as weak cytotoxicity in the HCT-116 and SW-480 human colon cancer cell lines with IC(50) values of 143 and 125 microM, respectively. While 1 was less active as an antioxidant than 2, the known compounds were more potent in the DPPH assay (IC(50) range 39.7-89.7 microM).

    Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Catechin; Colonic Neoplasms; Drug Screening Assays, Antitumor; Flavonoids; French Guiana; Glycosides; Humans; Inhibitory Concentration 50; Malvaceae; Molecular Structure; Picrates; Seeds; Tumor Cells, Cultured

2003
Structural studies on bioactive compounds. 23. Synthesis of polyhydroxylated 2-phenylbenzothiazoles and a comparison of their cytotoxicities and pharmacological properties with genistein and quercetin.
    Journal of medicinal chemistry, 1994, May-27, Volume: 37, Issue:11

    A series of polyhydroxylated 2-phenylbenzothiazoles 3 has been prepared by demethylation of the precursor methoxylated 2-phenylbenzothiazoles 9. The key step in the construction of the benzothiazole nucleus involves a Jacobson cyclization of methoxylated thiobenzanilides 8. The target compounds inhibit WiDr human colon tumor cells and MCF-7 human mammary tumor cells in vitro with IC50 values in the low micromolar range, but the activity against MCF-7 cells is not related to estrogen receptor-binding affinity. None of the compounds showed selective cytotoxicity against Abelson virus-transformed ANN-1 cells encoded with the pp120gag-abl tyrosine kinase compared with the parental 3T3 line. Compounds were only marginally inhibitory to the EGF receptor-associated protein tyrosine kinase from a membrane preparation of A431 cells. The most active compound was 4,6-dihydroxy-2-(4-hydroxyphenyl)benzothiazole (3b) which has the same overall hydroxyl substitution pattern as genistein (1a). The compounds were weakly cytotoxic for an EGF receptor, overexpressing cell line HN5, but when tested for differential toxicity against the EGF receptor tyrosine kinase or the PDGF receptor tyrosine kinase in a standard mitogenesis assay utilizing human fibroblasts, no discrimination was observed. In this assay, the compounds inhibited DNA synthesis when added to cells during S phase. This suggests that inhibition could not be interpreted in terms of tyrosine kinase inactivation but more likely as a relatively broad specificity for the ATP-binding domain of other kinases such as thymidine kinase.

    Topics: 3T3 Cells; Animals; Antineoplastic Agents; Breast Neoplasms; Cell Division; Colonic Neoplasms; ErbB Receptors; Fibroblasts; Genistein; Humans; Hydroxylation; Isoflavones; Mice; Molecular Structure; Protein-Tyrosine Kinases; Quercetin; Structure-Activity Relationship; Thiazoles; Tumor Cells, Cultured

1994