Synthesis, molecular modelling studies of artemisinin-chalcone derivatives and their antimalarial activity evaluation.

Twenty-two monomers and dimers of artemisinin having chalcone as a linker were synthesised, and their antimalarial activity against was determined, and a quantitative structure-activity relationship (QSAR) was developed. Artemisinin is a frontline antimalarial drug known worldwide but is threatened because of the rapidly emerging artemisinin-resistant strain , antimalarial IC (half-maximal inhibitory concentration) activity of a molecule against malaria parasites provides a good first screen for identifying the antimalarial potential of a particular molecule. The most active compound was artemisinin dimer dimethoxy chalcone as a linker with IC of 4.

Synthesis, molecular modelling studies of indolyl chalcone derivatives and their antimalarial activity evaluation.

Twenty one chalcone derivatives were synthesized using Claisen-Schmidt condensation, their antimalarial activity against was determined and quantitative structure-activity relationship (QSAR) was developed. Condensation of substituted acetophenones with various aromatic aldehydes at room temperature gave chalcones in 75-96% yield. Chalcones are secondary metabolites of terrestrial plants, precursors for the biosynthesis of flavonoids and exhibit various biological activities.

antiproliferative activity of glabridin derivatives and their target identification.

Novel Mannich base derivatives of glabridin were synthesized and their antiproliferative activity were performed along with our previously reported glabridin-chalcone hybrids molecules (GCHMs) against various human cell lines MDA-MB-231 (breast adenocarcinoma), HEK-293 (embryonic kidney cell line), K562 (leukemia), MCF-7 (breast adenocarcinoma), HeLa (cervix adenocarcinoma), HepG2 (hepatocellular carcinoma) and WRL-68 (hepatic carcinoma). The result showed that the glabridin significantly reduced cell proliferation with IC ranges from 3.67 to 58.

A novel bi-functional chalcone inhibits multi-drug resistant Staphylococcus aureus and potentiates the activity of fluoroquinolones.

Staphylococcus aureus is the leading cause of bacteraemia and the dwindling supply of effective antibacterials has exacerbated the problem of managing infections caused by this bacterium. Isoliquiritigenin (ISL) is a plant flavonoid that displays therapeutic potential against S. aureus.

Drug Resistance Reversal Potential of Isoliquiritigenin and Liquiritigenin Isolated from Glycyrrhiza glabra Against Methicillin-Resistant Staphylococcus aureus (MRSA).

Isoliquiritigenin (ISL) and liquiritigenin (LTG) are structurally related flavonoids found in a variety of plants. Discovery of novel antimicrobial combinations for combating methicillin-resistant Staphylococcus aureus (MRSA) infections is of vital importance in the post-antibiotic era. The present study was taken to explore the in vitro and in vivo combination effect of LTG and ISL with β-lactam antibiotics (penicillin, ampicillin and oxacillin) against mec A-containing strains of MRSA.

Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.

A new series of monomer and dimer derivatives of dihydroartemisinin (DHA) containing substituted chalcones as a linker were synthesized and investigated for their cytotoxicity in human cancer cell lines HL-60 (leukemia), Mia PaCa-2 (pancreatic cancer), PC-3 (prostate cancer), LS180 (colon cancer) and HEPG2 (hepatocellular carcinoma). Some of these derivatives have greater antiproliferative and cytotoxic effects in tested cell lines than parent compound DHA. The structures of the all compounds were confirmed by IR, (1)H NMR and mass spectral data.

Molecular modeling based synthesis and evaluation of in vitro anticancer activity of indolyl chalcones.

A series of twenty one chalcone derivatives having indole moiety were synthesized and were evaluated against four human cancer cell lines. Indolyl chalcones 1a, 1b, 1d, 1f-1j, 2c, 2e, 2i showed good anticancer activity. Chalcones 1b and 1d were the most active and selective anticancer agents with IC50 values <1μg/ml and 1.

Molecular modeling based semi-synthesis and in vitro evaluation of anticancer activity in indolyl chalcones.

A series of indolyl chalcones were synthesized and evaluated in vitro for their anticancer activity against four human cancer cell lines. Compounds 1a, 1b, 1d, 1f-1j, 2c, 2e, 2i showed significant cytotoxicity. Chalcones 1b and 1d were identified as the most potent and selective anticancer agents with IC50 values <1µg/ml and 1.

In vitro antimalarial studies of novel artemisinin biotransformed products and its derivatives.

Biotransformation of antimalarial drug artemisinin by fungi Rhizopus stolonifer afforded three sesquiterpenoid derivatives. The transformed products were 1α-hydroxyartemisinin (3), 3.0%, a new compound, 10β-hydroxyartemisinin, 54.

QSAR and docking based semi-synthesis and in vivo evaluation of artemisinin derivatives for antimalarial activity.

To screen the active antimalarial novel artemisinin derivatives, a QSAR modeling approach was used. QSAR model showed high correlation (r(2)= 0.83 and rCV(2)= 0.

In vivo anti-diabetic activity of derivatives of isoliquiritigenin and liquiritigenin.

Isoliquiritigenin (ISL), a chalcone and liquiritigenin (LTG), a flavonoid found in licorice roots and several other plants. ISL displays antioxidant, anti-inflammatory, antitumor and hepatoprotective activities whereas LTG is an estrogenic compound, acts as an agonist selective for the β-subtype of the oestrogen receptor. Both the phenolics were isolated from the rhizomes of Glycyrrhiza glabra.

Antimalarial drug targets and drugs targeting dolichol metabolic pathway of Plasmodium falciparum.

Because of mutation and natural selection, development of drug resistance to the existing antimalarial is the major problem in malaria treatment. This problem has created an urgent need of novel antimalarial drug targets as well as lead compounds. The important characteristic of malaria is that it shows the phenomenon of balanced polymorphisms.

Antiplasmodial activity of artecyclopentyl mether a new artemisinin derivative and its effect on pathogenesis in Plasmodium yoelii nigeriensis infected mice.

In an effort to evaluate novel derivatives from artemisinin, possessing potential antimalarial activity, a new derivative artecyclopentyl mether (CPM-1) was derivatized and evaluated for its dose-dependent efficacy in Plasmodium yoelii nigeriensis infected mice. The survivability of mice at 7.5 mg/kg was >28 days with negligible parasitaemia and recovered anemia (66.

Liquiritigenin derivatives and their hepatotoprotective activity.

Liquiritigenin (7,4'-dihydroxyflavanone), isolated from the roots of Glycyrrhiza glabra, was derivatized to liquiritigenin 7, 4'-diacetate, liquiritigenin 4'-acetate, isoliquiritigenin, and liquiritigenin 7, 4'-dibenzoate. All these derivatives were evaluated for in vitro hepatoprotective activity against D-galactosamine-lipopolysaccharide(GalN/LPS) induced toxicity. In-vitro hepatotoxicity was manifested by a significant increase (P < 0.