Synthesis and biological evaluation of scopoletin derivatives

Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.

ГлавнаяSynthesis And Antitumor Activity Of Scopoletin Derivatives

Aline Witaicenis et al evaluated antioxidant activity 31 of some plant derived coumarins (scopoletin, scoparone, fraxetin, 4-methyl-umbeliferone, esculin and daphnetin) (Fig.23) to verify if potential intestinal anti inflammatory activity was related to anti oxidant activity. Two in vitro assays were used to test the antioxidant activity of the coumarin derivatives: the lipid peroxidation in rat brain membranes and DPPH assays.

Synthesis, biological evaluation and docking studies of …

Bylov et al synthesized 30 a series of N-aryl substituted 2-imino-2H-1-benzopyran-3-carboxamide and 2-oxo-2H-1-benzopyran-3-carboxamide and evaluated them for anti inflammatory in carageenan induced rat paw oedema and in acetic acid peritonitis test in albino rats. The results were found to be comparable with piroxicam taken as reference drug. In the consideration of the efficacy of the compounds in these assays, 2-imino/oxo-2H-1-benzopyran-3-carboxamides were further studied at graded doses for their acute toxicities (ALD50) in albino mice and were found to be essentially non toxic at highest dose test.

Roussaki et al synthesized 33 a series of coumarin analogues bearing a substituted phenyl ring on position 3 via a novel methodology through an intermolecular condensation reaction of 2-hydroxyacetophenone and 2-hydroxybenzaldehyde with imidazoylphenylacetic acid active intermediate. In vitro antioxidant activity of synthesized derivatives was evaluated using two different antioxidant assays (radical scavenging ability of DPPH stable free radicals and inhibition of lipid peroxidation induced by thermal free radical AAPH). Ability of compounds, (Fig. 24) to inhibit soybean lipoxygenase was also determined as an indication of potential anti inflammatory activity.


Synthesis and biological evaluation …

"PASS prediction of antibacterial activity of dihydropyrimidinones derivatives has been confirmed by the synthesis and biological testing against S. Aureus and S. Typhi bacteria. Moreover, PASS predicted antineoplastic action indicates the directions for further testing of the synthesized compounds."

Synthesis, biological evaluation and 3D-QSAR studies ..

"According to PASS, a tool for estimation of potential pharmacological effects and biological targets, the synthesized molecules {N-alkylated C-6-isobutyl- or -propyl pyrimidine derivatives} were predicted to have antiviral activity what is in accordance with the observed antiviral activities of some C-6 substituted thymine and uracil derivates. However, different target molecules for pyrimidin-2,4-dione and 2,4-dimethoxypyrimidine derivatives were suggested as the most probable by PASS. Although both classes have shown antiproliferative effects, their modes of action at molecular level may differ according to PASS. … Predicted inhibition of cell adhesion might explain the strong antiproliferative effect observed on adherent tumor cell lines. It has already been shown that binding of tumor cells to extracellular matrix proteins might promote tumor invasiveness, that is, binding of metastatic colon cancer cells to fibrinogen or breast cancer cells to fibronectin. Adhesion analysis for adherent tumor cells on the fibronectin matrix confirmed that adhesion molecules are indeed, targeted by compound 14b. It was evident that adhesion of all tested cell lines was strongly affected by treatment with compound 14b."

Synthesis and biological evaluation of scopoletin derivatives.

Reddy NS et al. synthesized coumarin 3-(N-aryl) sulphonamides 41 (Fig. 31). The effect of all the compounds on the growth of human tumor cells in culture was evaluated using androgen receptor negative prostate (DU145), colorectal (DLD-1), non-small cell lung carcinoma (H157), estrogen receptor negative breast (BT20), and chronic myeloid leukemia (K562) cell lines. The dose response of each cell line was established by determining the number of viable cells after 96 hours of continuous treatment against five different concentrations (1-100 μM range) of each compound. The activation of JNK1 by these compounds as shown in immune complex kinase assay, clearly showed that they activate JNK pathway either by interacting with JNK1 or with one of the upstream kinases in this pathway 42.

synthesis, biological evaluation and ..


Abstract In an effort to discover potent camptothecin-derived antitumor agents, novel camptothecin analogues with sulfonylpiperazinyl motifs at position-7 were designed and synthesized. They were evaluated for in vitro cytotoxicity with the sulforhodamine-B (SRB) method in five types of human tumor cell lines, A-549, MDA-MB-231, KB, KB-VIN and MCF-7. With IC50 values in the low μM to nM level, most of the new analogues showed greater cytotoxicity activity than the reference compounds irinotecan and topotecan. Furthermore, compounds 12l (IC50, 1.2nM) and 12k (IC50, 20.2nM) displayed the highest cytotoxicity agai...