Synthesis and pharmacological activities of xanthone derivatives as α-glucosidase inhibitors

Compounds of Formula (I) that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.

Materials and methods to potentiate cancer treatment

Rhein, an active ingredient extensively found in plants such as Aloe, Cassitora L., rhubarb and so on, has been used for a long time in China. Pharmacological tests revealed that rhein not only had a strong antibacterial action, but also may be useful in cancer chemotherapy as a biochemical modulator. Its therapeutic action and toxicity is still the subject of considerable research. With microsome incubation assays in vitro and HPLC methods, the inhibition of rat liver CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A enzymes by rhein were studied kinetically. The results showed the most inhibition of CYP2E1 by rhein (K(i) = 10 microm, mixed); CYP3A and CYP2C9 were also inhibited by rhein, K(i) = 30 microm (mixed) and K(i) = 38 microm (mixed), respectively; rhein revealed some inhibition of CYP1A2 (K(i) = 62 microm, uncompetitive) and CYP2D6 (K(i) = 74 microm, mixed). Drug-drug interactions, especially cytochrome P450 (CYP)-mediated interactions, cause an enhancement or attenuation in the efficacy of co-administered drugs. Inhibition of the five major CYP enzymes observed for rhein suggested that changes in pharmacokinetics of co-administered drugs were likely to occur. Therefore, caution should be paid to the possible drug interaction of medicinal plants containing rhein and CYP substrates.

Inhibition of cytochrome P450 enzymes by rhein in rat liver microsomes.

Introduction: H+/K+-ATPase is a P-type ATP-driven cation transporter which exchanges ions (protons, chloride ions, and potassium ions) across the cell membrane. Modulators of H+/K+-ATPase affect H+/K+ exchange. Areas covered: This article describes various H+/K+-ATPase inhibitors of biological importance in clinical studies and drug development for gastric acid-related diseases and gastrointestinal disorders. Expert opinion: H+/K+-ATPase modulators have attracted much interest for their clinical implication in gastric acid-related diseases. Future studies of gastric H+/K+-ATPase inhibitors may focus on the correlation of pharmacogenetics and pharmacogenomics with the gastric acid secretion and development of more effective H+/K+-ATPase inhibitors to increase their residence time such as tenatoprazole and novel chemical-mediated absorption chemicals. The K+-competitive acid pump antagonists (APAs) are invented and independent of an acidic environment with better inhibition of the pump rapidly control acid ...

H+/K+-ATPase inhibitors: a patent review.

Synthesis and characterization of the Zn(II) and Cu(II) piperidinyl isoeuxanthone complexes: DNA-binding and cytotoxic activity.

Synthesis of quinone and xanthone analogs of rhein

The invention concerns phenoxy-isobutyric acid derivatives of general formula (I) wherein: R1 and R2 are H, an alkyl group, or a -OR group where R is an alkyl, or R1 and R2 together form a hydrocarbon ring of 3 to 6 carbon atoms; R3 is H or an alkyl group; X is O-, -S- or-CH2-; R4 is H, a halogen or -CF3, -OCH3, -CH3, -SCH3; Y is -CH2CH2-, CH=CH- or -C≡C-; Z1 is -O- or -NR6- or R6 is H or an alkyl group of 1 to 6 carbon atoms; Z2 is - (C=O ) -, - ( C=S ) - or - ( SO2 ) -; Z3 is a R5, - (NH-R5) or - (OR5) group, R5 being a 5- to 7-membered cycloalkyl group or a [- (CH2) m-aryl] group, with m = 0 or 1, or a heterocyclic group. The invention is useful for treating type II diabetes, hyperlipidemias and atherosclerosis.

Ppar enhancing derivatives, method for preparing same and therapeutic use thereof

The invention concerns novel flavone and isoflavone derivatives of formulae (Ia) and (Ib) wherein: X represents a group of formula -COOR, or -PO(OR)2; R represents a hydrogen atom or an alkaline or alkaline-earth metal, or a lower alkyl group; R1 represents a hydroxy group, a lower alkoxy group or an acyloxy group; R2 and R3, identical or different, represent a hydrogen or halogen atom, or a trifluoromethyl group, a trichloromethyl group, a hydroxy group, an alkoxy group or an acyloxy group comprising 1 to 5 carbon atoms, or R2 and R3 can combine to form an alkylene dioxy group. The invention is useful for treating rheumatic diseases.

7-carboxy-flavone derivatives, preparation method and therapeutic use

The invention relates to a tenatoprazole sodium monohydrate salt of formula (I) and to the therapeutic use thereof for treating digestive pathologies.

Herve Ficheux

Papers

Synthesis of quinone and xanthone analogs of rhein

Ppar enhancing derivatives, method for preparing same and therapeutic use thereof

7-carboxy-flavone derivatives, preparation method and therapeutic use

S-tenatoprazole sodium monohydrate salt and the use thereof in the form of a proton pump inhibitor

The use of tenatoprazole in the treatment of gastroesophageal reflux disease