Compounds > 3-hydroxy-4-3--4--5--tetramethoxychalcone

3-hydroxy-4-3--4--5--tetramethoxychalcone and fosbretabulin

3-hydroxy-4-3--4--5--tetramethoxychalcone has been researched along with fosbretabulin* in 2 studies

Other Studies

2 other study(ies) available for 3-hydroxy-4-3--4--5--tetramethoxychalcone and fosbretabulin

Article	Year
A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent. Bioorganic & medicinal chemistry, 2010, Jan-15, Volume: 18, Issue:2 Chalcones represent a class of natural products that inhibits tubulin assembly. In this study we designed and synthesized boronic acid analogs of chalcones in an effort to compare biological activities with combretastatin A-4, a potent inhibitor of tubulin polymerization. Systematic evaluation of the positional effects of the carbonyl moiety towards inhibition of tubulin polymerization, cancer cell proliferation and angiogenesis revealed that placement of the carbonyl adjacent to the trimethoxybenzene A-ring resulted in more active compounds than when the carbonyl group was placed adjacent to the C-ring. Our study identified a boronic acid chalcone with inhibition towards 16 human cancer cell lines in the 10-200nM range, and another three cell lines with GI(50)-values below 10nM. Furthermore, this drug has significant anti-angiogenesis effects demonstrated by HUVEC tube formation and aortic ring assay. Topics: Antineoplastic Agents; Boronic Acids; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Chalcone; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Endothelial Cells; Humans; Molecular Structure; Stereoisomerism; Stilbenes; Structure-Activity Relationship	2010
Pt(II) complexes of a combretastatin A-4 analogous chalcone: effects of conjugation on cytotoxicity, tumor specificity, and long-term tumor growth suppression. Journal of medicinal chemistry, 2009, Jan-22, Volume: 52, Issue:2 Three dichlorido(6-aminomethylnicotinate)platinum complexes 6 comprising a combretastatin A-4 analogous chalcone were tested on a panel of 21 tumor cell lines from 9 entities. Parent chalcone 1a and the directly linked conjugate 6a exhibited excellent antiproliferative activities, similar in magnitude [average log(IC(50)) values of -7.3 (1a) and -7.0 (6a)] and cell line specificity but slightly different in the mechanism of apoptosis induction. While 1a and 6a caused an equally fast rise in caspase-9 in the tested cancer cell lines, the downstream effector caspase-3 built up faster in cells treated with 1a compared to 6a, yet reached an equal end level. They also had different long-term effects on the regrowth of cancer cells treated with a single dose. In contrast, conjugates 6b,c featuring longer spacers between the Pt complex and the chalcone moieties were less antiproliferative than 6a. Topics: Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Chalcones; Dose-Response Relationship, Drug; Humans; Platinum; Stilbenes	2009

Article

Year

A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent.

Bioorganic & medicinal chemistry, 2010, Jan-15, Volume: 18, Issue:2

Chalcones represent a class of natural products that inhibits tubulin assembly. In this study we designed and synthesized boronic acid analogs of chalcones in an effort to compare biological activities with combretastatin A-4, a potent inhibitor of tubulin polymerization. Systematic evaluation of the positional effects of the carbonyl moiety towards inhibition of tubulin polymerization, cancer cell proliferation and angiogenesis revealed that placement of the carbonyl adjacent to the trimethoxybenzene A-ring resulted in more active compounds than when the carbonyl group was placed adjacent to the C-ring. Our study identified a boronic acid chalcone with inhibition towards 16 human cancer cell lines in the 10-200nM range, and another three cell lines with GI(50)-values below 10nM. Furthermore, this drug has significant anti-angiogenesis effects demonstrated by HUVEC tube formation and aortic ring assay.

Topics: Antineoplastic Agents; Boronic Acids; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Chalcone; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Endothelial Cells; Humans; Molecular Structure; Stereoisomerism; Stilbenes; Structure-Activity Relationship

2010

Pt(II) complexes of a combretastatin A-4 analogous chalcone: effects of conjugation on cytotoxicity, tumor specificity, and long-term tumor growth suppression.

Journal of medicinal chemistry, 2009, Jan-22, Volume: 52, Issue:2

Three dichlorido(6-aminomethylnicotinate)platinum complexes 6 comprising a combretastatin A-4 analogous chalcone were tested on a panel of 21 tumor cell lines from 9 entities. Parent chalcone 1a and the directly linked conjugate 6a exhibited excellent antiproliferative activities, similar in magnitude [average log(IC(50)) values of -7.3 (1a) and -7.0 (6a)] and cell line specificity but slightly different in the mechanism of apoptosis induction. While 1a and 6a caused an equally fast rise in caspase-9 in the tested cancer cell lines, the downstream effector caspase-3 built up faster in cells treated with 1a compared to 6a, yet reached an equal end level. They also had different long-term effects on the regrowth of cancer cells treated with a single dose. In contrast, conjugates 6b,c featuring longer spacers between the Pt complex and the chalcone moieties were less antiproliferative than 6a.

Topics: Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Chalcones; Dose-Response Relationship, Drug; Humans; Platinum; Stilbenes

2009