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Synthesis and biological evaluation of new curcumin analogues as antioxidant and antitumor agents: molecular modeling study.
Bayomi, Said M; El-Kashef, Hassan A; El-Ashmawy, Mahmoud B; Nasr, Magda N A; El-Sherbeny, Magda A; Abdel-Aziz, Naglaa I; El-Sayed, Magda A-A; Suddek, Ghada M; El-Messery, Shahenda M; Ghaly, Mariam A.
Afiliación
  • Bayomi SM; Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • El-Kashef HA; Department of Pharmacology, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • El-Ashmawy MB; Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • Nasr MN; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • El-Sherbeny MA; Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • Abdel-Aziz NI; Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • El-Sayed MA; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • Suddek GM; Department of Pharmacology, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • El-Messery SM; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
  • Ghaly MA; Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt. Electronic address: mariamaghaly2@yahoo.com.
Eur J Med Chem ; 101: 584-94, 2015 Aug 28.
Article en En | MEDLINE | ID: mdl-26197162
New curcumin analogues have been synthesized and their antioxidant activities were investigated by measuring their free radical scavenging capacities. The in vitro and in vivo antitumor activities of the synthesized compounds on Ehrlich ascites carcinoma (EAC) cell line were evaluated. 4-(4-Chlorophenyl)-2-(5-ethyl-7-(4-methoxybenzylidene)-3-(4-methoxyphenyl)-3,3a,4,5,6,7-hexahydro-2H-pyrazolo[4,3-c] pyridin-2-yl)thiazole 7h showed excellent antineoplastic activity in both in vitro and in vivo studies more than that of tested compounds and reference drug, cisplatin. Different molecular modeling studies were performed, where docking of compound 7h into telomerase active site suggested that it could exert its antitumor potential by telomerase inhibition.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Carcinoma de Ehrlich / Curcumina / Antineoplásicos / Antioxidantes Límite: Animals / Female / Humans Idioma: En Revista: Eur J Med Chem Año: 2015 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Francia

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Carcinoma de Ehrlich / Curcumina / Antineoplásicos / Antioxidantes Límite: Animals / Female / Humans Idioma: En Revista: Eur J Med Chem Año: 2015 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Francia