Sixteen antimalarial alkoxylated and hydroxylated chalcones were tested for their ability to inhibit recombinant plasmepsin II in vitro. The best inhibitory compounds had either a chloro or dimethylamino group at the 4-position of phenyl ring A in the chalcone template. Combination of the chalcones with chloroquine showed additivity or mild antagonism of Plasmodium falciparum K1 growth in culture.

Cervical cancer is the second leading cause of death in women. Many treatments currently provide toxic effects on normal cells. Therefore, alternative treatment using chalcone derivatives has potent anticancer properties that can help reduce side effects. Chalcone with halogen and methoxy groups ring B potentially inhibit This research aimed to synthesize halogen-substituted by a green chemistr...

In the title chalcone [systemetic name 1-(2,4-dimeth-oxy-phen-yl)-3-(3,4,5-trimeth-oxy-phen-yl)prop-2-en-1-one], C(20)H(22)O(6), the dihedral angle between the plane of the two benzene rings is 7.03 (4)° with all but one of the meth-oxy groups essentially co-planar with these rings [C-C-O-C torsion angles = -76.1 (2), -0.7 (3), 1.8 (3), -6.2 (3), 2.0 (3)°]. An intra-molecular C-H⋯O inter-action...

The title compound, C(16)H(12)F(3)NO, a derivative of biologically active chalcones, comprises two benzene rings and a central -CH=CH-C(=O)- unit. The dihedral angle between the two rings is 10.9 (1)° and the mol-ecule adopts an E configuration about the central olefinic bond. The crystal structure is stabilized by inter-molecular N-H⋯O and N-H⋯N hydrogen bonds.

  Objective(s): Chalcones and their rigid analogues represent an important class of small molecules having anticancer activities. Therefore, in this study the synthesis and cytotoxic activity of new 3-benzylidenchroman-4-ones were described as rigid chalcone analogues.   Materials and Methods: The reaction of resorcinol with 3-chloropropionic acid in the presence of CF3SO3H was a...

Chalcones and dihydrochalcones exhibit chemopreventive and antitumor activity. TRAIL (tumor necrosis factor-related apoptosis-inducing ligand) is a natural endogenous anticancer agent. We examined the cytotoxic and apoptotic effect of chalcones and dihydrochalcones on TRAIL-mediated apoptosis in LNCaP prostate cancer cells. The cytotoxicity was evaluated by the MTT and LDH assays. The apoptosis...

We have synthesized four novel derivatives of podophyllotoxin, the chalcone derivatives namely 2benzylidene-6,7-dimethoxy-4-phenyl-3,4-dihydro-2H-naphthalen-1-one (4a), 2-benzylidene-5,7-dichloro-6hydroxy-4-phenyl-3,4-dihydro-2H-naphthalen-1-one(4b), and the amino-thiazolyl derivatives namely7,8dimethoxy-5-phenyl-4,5-dihydro-naphtha[1,2-d] thiazol-2-yl amine (5a) and 2-amino-6,8-dichloro-5-phen...

2- Ethoxy-4(3H) quinazolinone 1 was synthesized and allowed to react with various halides, namely: alkyl, benzyl, allyl, acyl, haloacetyl, crotonyl, benzoyl, 2-furoyl and 1-naphthalenesulphonyl halides affording quinazoline and quinazolinone derivatives. The reactions of compound 1 with phosphorus oxychloride, phosphorus pentasulfide, ethyl chloroformate, ethyl chloroacetate, ?-bromoglucose tet...