Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3K&#945;/mTOR inhibitors.

Al-Ashmawy, Aisha A K; Ragab, Fatma A; Elokely, Khaled M; Anwar, Manal M; Perez-Leal, Oscar; Rico, Mario C; Gordon, John; Bichenkov, Eugeney; Mateo, George; Kassem, Emad M M; Hegazy, Gehan H; Abou-Gharbia, Magid; Childers, Wayne

Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3Kα/mTOR inhibitors.

Al-Ashmawy, Aisha A K; Ragab, Fatma A; Elokely, Khaled M; Anwar, Manal M; Perez-Leal, Oscar; Rico, Mario C; Gordon, John; Bichenkov, Eugeney; Mateo, George; Kassem, Emad M M; Hegazy, Gehan H; Abou-Gharbia, Magid; Childers, Wayne.

Afiliação

Al-Ashmawy AAK; Moulder Center for Drug Discovery Research, Temple University, School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, USA; Department of Therapeutical Chemistry, National Research Center, Dokki, Cairo 12622, Egypt.
Ragab FA; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo 11562, Egypt.
Elokely KM; Department of Pharmaceutical Chemistry, Tanta University, Tanta 31527, Egypt; Department of Chemistry and ICMS, Temple University, Philadelphia 19122, PA, USA.
Anwar MM; Department of Therapeutical Chemistry, National Research Center, Dokki, Cairo 12622, Egypt.
Perez-Leal O; Moulder Center for Drug Discovery Research, Temple University, School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, USA.
Rico MC; Moulder Center for Drug Discovery Research, Temple University, School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, USA.
Gordon J; Moulder Center for Drug Discovery Research, Temple University, School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, USA.
Bichenkov E; Moulder Center for Drug Discovery Research, Temple University, School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, USA.
Mateo G; Moulder Center for Drug Discovery Research, Temple University, School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, USA.
Kassem EMM; Department of Therapeutical Chemistry, National Research Center, Dokki, Cairo 12622, Egypt.
Hegazy GH; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo 11562, Egypt.
Abou-Gharbia M; Moulder Center for Drug Discovery Research, Temple University, School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, USA.
Childers W; Moulder Center for Drug Discovery Research, Temple University, School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, USA. Electronic address: wchilders@yahoo.com.

Bioorg Med Chem Lett ; 27(14): 3117-3122, 2017 07 15.

Article em En | MEDLINE | ID: mdl-28571824

Assuntos

Antineoplásicos/síntese química; Desenho de Fármacos; Inibidores de Fosfoinositídeo-3 Quinase; Pirimidinas/química; Serina-Treonina Quinases TOR/antagonistas & inibidores; Trifosfato de Adenosina/química; Trifosfato de Adenosina/metabolismo; Antineoplásicos/química; Antineoplásicos/farmacologia; Sítios de Ligação; Ligação Competitiva; Linhagem Celular Tumoral; Sobrevivência Celular/efeitos dos fármacos; Classe I de Fosfatidilinositol 3-Quinases; Humanos; Concentração Inibidora 50; Células MCF-7; Simulação de Acoplamento Molecular; Fosfatidilinositol 3-Quinases/metabolismo; Estrutura Terciária de Proteína; Pirimidinas/síntese química; Pirimidinas/farmacologia; Relação Estrutura-Atividade; Serina-Treonina Quinases TOR/metabolismo

Palavras-chave

3-Kinase alpha; Dual inhibitor; Pyrido[2,3-d]pyrimidine phosphoinositide; Pyrido[3,2-d]pyrimidine; mTOR

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Desenho de Fármacos / Serina-Treonina Quinases TOR / Inibidores de Fosfoinositídeo-3 Quinase / Antineoplásicos Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Ano de publicação: 2017 Tipo de documento: Article

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