Design, in silico studies, synthesis, and in vitro anticancer assessment of new naphthylidene isoxazolidinedione derivatives

Cancer is the most destructive and fatal disease, representing an urgent medical challenge to the world. The discovery of a new anticancer candidate may help reduce or eliminate this alarming disease to a greater extent. On similar lines, in silico research was carried out on novel naphthylidene isoxazolidinedione derivatives that were logically conceived, synthesized, purified, and structurally characterized. In vitro biological evaluation revealed the most active compound 4d with an inhibitory concentration of 42.87 mu m against K562 and 47.42 mu m on A549 cells. The anticancer activity of this naphthylidene isoxazolidinedione derivative was evident by cell cycle and apoptosis assays, which showed arrest of the G2/M phase (65.6%) of the K562 cells and induction of apoptosis with 21.47% apoptotic cells as compared to 0.2% of untreated cells, respectively. image

Авторы
Upadhyay N. 1 , Tilekar K. 1 , Oak A. 1 , Pokrovsky V.S. 2, 3 , Chelakara R.S. 1
Издательство
WILEY
Номер выпуска
2
Язык
Английский
Страницы
217-226
Статус
Опубликовано
Том
62
Год
2024
Организации
  • 1 Bharati Vidyapeeths Coll Pharm, Dept Pharmaceut Chem, Navi Mumbai 400614, India
  • 2 NN Blokhin Canc Res Ctr, Lab Biochem Fundamentals Pharmacol & Canc Models, Moscow, Russia
  • 3 Peoples Friendship Univ, Dept Biochem, Moscow, Russia
Ключевые слова
antiproliferative; apoptosis; bio-isostere; cell cycle; isoxazolidinedione
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