Phenylpropiophenone derivatives as potential anticancer agents: Synthesis, biological evaluation and quantitative structure–activity relationship study

Procognitive Properties of Drugs with Single and Multitargeting H3 Receptor Antagonist Activities

“…Results obtained from our previous theoretical studies, pharmacophore modeling, design , synthesis, and biological evaluation of novel compounds should be further used in discovery of novel dual‐activity hH 3 R antagonists/inverse agonists with procognitive effect.…”

Chalcone derivative cytotoxicity activity against MCF-7 human breast cancer cell QSAR study

“…The same authors synthesized metoxylated chalcones with N-methyl substituents on ring A and showed inhibition of the growth of the MCF7 cell lines, because piperidinyl group adds specificity to the mechanism of activity and also changes physiochemical properties of the whole system [11]. In a study by Ivkovic et al [4] some of the basic modifications of the chalcone structure were introduced, for example electron withdrawing groups (-F, -Cl and -CF 3 ) in the ortho and para position in the benzyl moiety and their antiproliferative activity was investigated, and structure-activity analysis was performed in order to determine the best molecular descriptors for this class of chalcones.…”

“…In our QSAR study, a total of 93 chalcone molecules were gathered from the literature [4,[10][11][12]. To our knowledge this particular set of molecules was not employed in a QSAR study before.…”

“…1), present a very interesting group of molecules from pharmaceutical point of view, because of their significant cytotoxic activity against various cancer cells. Besides this important feature chalcones and their analogues display considerable chemoprotective, antiangiogenic, antibacterial, antifugal, antiparasitic, antioxidative, anti-inflammatory activity [4,5] and antimarial activity [6,7]. Chalcones are also precursors for synthesis of flavonoids, which are also known for their anticancer potential [8].…”

“…Some of the main problems in the treatment of cancer are high cytotoxicity and drug resistance, and no clinically active substances are known to act selectively on tumor cells. Scientists put great effort in finding new therapeutic targets for cancer and to the development of new selective drugs [4].…”