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Relevant academic research and scientific papers

Synthesis of diaryl urea derivatives and evaluation of their antiproliferative activities in colon adenocarcinoma

Colon cancer is one of the leading causes of cancer-related deaths today. Serious research for ideal chemotherapy continues today. In this context, newly synthesized molecules have an essential role in cancer treatment research. The effects of 5 diaryl urea derivatives synthesized within the scope of this study on the HT-29 colon cancer cell line were investigated for the first time in the literature by in-silico and in-vitro methods. Among the five compounds produced in the first stage of the study, DAU5 was found to have a cytotoxic effect on HT-29. However, it was determined that it did not show a serious cytotoxic effect on L929 (healthy fibroblast cell line) at the same doses. The efficacy of DAU5 was evaluated for expression of LC3B, an indicator of autophagy, and 8-OHdG, an indicator of oxidative stress-DNA damage. LC3B and 8-OHdG expression were lower in the DAU5 treatment group than in the control group. As a result, it was seen that DAU5, a diaryl urea derivative compound we synthesized in this study, has the potential to be a chemotherapeutic agent against colon cancer. However, our study needs to be supported by in vivo and clinical studies.

Design, synthesis, and antitumor activity of novel sorafenib derivatives

New series of 18 compounds were synthesized using sorafenib derivatives as parent structure and p-aminoacetophenone as raw materials. The structures of the newly synthesized compounds were confirmed on the basis of 1H, 13C NMR and HR

Synthesis of new hydrazone derivatives and evaluation of their monoamine oxidase inhibitory activity

A novel series of hydrazone derivatives were designed and synthesized. Their structures were characterized by IR, 1H NMR, 13C NMR and HR-MS spectroscopic methods. The newly synthesized compounds were evaluated for their inhibitory ac

Synthesis and Biological Evaluation of Novel 1-(4-(Hydroxy(1-oxo-1,3-dihydro-2H-inden-2-ylidene)methyl)phenyl)-3-phenylurea Derivatives

A series of novel phenylurea containing 2-benzoylindan-1-one derivatives 3a?–?3j were synthesized from the reaction of phenylurea-substituted acetophenones 1a?–?1j with phthalaldehyde 2 under mild reaction conditions in good yields. All synthesized compou

Preparation method for alkyl/benzyl/aryl urea compounds through heterogeneous-phase catalysis

The invention discloses a preparation method for formula (I) compounds, and the compounds are obtained by reacting a formula (II) compound with a formula (III) compound in a solvent in carbon monoxide atmosphere under catalysis of a heterogeneous-phase pa

DIARYL UREAS AS CB1 ANTAGONISTS

Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.

Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives

Phenylurenyl chalcone derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-resistant strain of Plasmodium falciparum, activity of the cysteine protease falcipain-2, in vitro globin hydrolysis, β-hematin forma