Novel scaffold hopping of potent benzothiazole and isatin analogues linked to 1,2,3-triazole fragment that mimic quinazoline epidermal growth factor receptor inhibitors: Synthesis, antitumor and mechanistic analyses.

Rezki, Nadjet; Almehmadi, Meshal A; Ihmaid, Saleh; Shehata, Ahmed M; Omar, Abdelsattar M; Ahmed, Hany E A; Aouad, Mohamed Reda

Rezki, Nadjet; Almehmadi, Meshal A; Ihmaid, Saleh; Shehata, Ahmed M; Omar, Abdelsattar M; Ahmed, Hany E A; Aouad, Mohamed Reda.

Afiliação

Rezki N; Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Munawarah 30002, Saudi Arabia. Electronic address: nadjetrezki@yahoo.fr.
Almehmadi MA; Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Munawarah 30002, Saudi Arabia.
Ihmaid S; Pharmacognosy and Pharmaceutical Chemistry Department, College of Pharmacy, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia.
Shehata AM; Pharmacology and Toxicology Department, College of Pharmacy, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia; Department of Pharmacology and Toxicology, Faculty of Pharmacy, Beni-Suef University, Egypt.
Omar AM; Pharmaceutical Chemistry Department, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Nasr City 11884, Cairo, Egypt.
Ahmed HEA; Pharmacognosy and Pharmaceutical Chemistry Department, College of Pharmacy, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, 11884 Nasr City, Cairo, Egypt. Electronic address: heahmad@taibahu.edu.sa.
Aouad MR; Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Munawarah 30002, Saudi Arabia.

Bioorg Chem ; 103: 104133, 2020 10.

Article em En | MEDLINE | ID: mdl-32745759

Assuntos

Antineoplásicos/farmacologia; Benzotiazóis/farmacologia; Isatina/farmacologia; Inibidores de Proteínas Quinases/farmacologia; Quinazolinas/farmacologia; Triazóis/farmacologia; Antineoplásicos/síntese química; Antineoplásicos/química; Apoptose/efeitos dos fármacos; Benzotiazóis/síntese química; Benzotiazóis/química; Linhagem Celular Tumoral; Proliferação de Células/efeitos dos fármacos; Cristalografia por Raios X; Relação Dose-Resposta a Droga; Ensaios de Seleção de Medicamentos Antitumorais; Receptores ErbB/antagonistas & inibidores; Receptores ErbB/metabolismo; Humanos; Isatina/síntese química; Isatina/química; Modelos Moleculares; Estrutura Molecular; Inibidores de Proteínas Quinases/síntese química; Inibidores de Proteínas Quinases/química; Quinazolinas/química; Relação Estrutura-Atividade; Triazóis/química

Palavras-chave

Anticancer activity; Apoptosis; Benzothiazole; Cell cycle analysis; EGFR TK; Isatin; Triazole

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Quinazolinas / Triazóis / Inibidores de Proteínas Quinases / Benzotiazóis / Isatina / Antineoplásicos Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article

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