Discovery of amide-bridged pyrrolo[2,3-d]pyrimidines as tumor targeted classical antifolates with selective uptake by folate receptor &#945; and inhibition of de novo purine nucleotide biosynthesis.

Xiang, Weiguo; Dekhne, Aamod; Doshi, Arpit; O'Connor, Carrie; Hou, Zhanjun; Matherly, Larry H; Gangjee, Aleem

Discovery of amide-bridged pyrrolo[2,3-d]pyrimidines as tumor targeted classical antifolates with selective uptake by folate receptor α and inhibition of de novo purine nucleotide biosynthesis.

Xiang, Weiguo; Dekhne, Aamod; Doshi, Arpit; O'Connor, Carrie; Hou, Zhanjun; Matherly, Larry H; Gangjee, Aleem.

Afiliação

Xiang W; Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States.
Dekhne A; Department of Oncology, Wayne State University School of Medicine, Detroit, MI 48201, United States.
Doshi A; Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States.
O'Connor C; Department of Oncology, Wayne State University School of Medicine, Detroit, MI 48201, United States.
Hou Z; Department of Oncology, Wayne State University School of Medicine, Detroit, MI 48201, United States; Molecular Therapeutics Program, Barbara Ann Karmanos Cancer Institute, 421 E. Canfield Street, Detroit, MI 48201, United States.
Matherly LH; Department of Oncology, Wayne State University School of Medicine, Detroit, MI 48201, United States; Department of Pharmacology, Wayne State University School of Medicine, Detroit, MI 48201, United States; Molecular Therapeutics Program, Barbara Ann Karmanos Cancer Institute, 421 E. Canfield Street,
Gangjee A; Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States. Electronic address: gangjee@duq.edu.

Bioorg Med Chem ; 27(23): 115125, 2019 12 01.

Article em En | MEDLINE | ID: mdl-31679978

Assuntos

Antineoplásicos/química; Antineoplásicos/farmacologia; Antagonistas do Ácido Fólico/química; Antagonistas do Ácido Fólico/farmacologia; Piridinas/química; Piridinas/farmacologia; Pirróis/química; Pirróis/farmacologia; Amidas/química; Amidas/farmacocinética; Amidas/farmacologia; Animais; Antineoplásicos/farmacocinética; Vias Biossintéticas/efeitos dos fármacos; Células CHO; Linhagem Celular Tumoral; Cricetulus; Receptor 1 de Folato/metabolismo; Antagonistas do Ácido Fólico/farmacocinética; Humanos; Modelos Moleculares; Neoplasias/tratamento farmacológico; Neoplasias/metabolismo; Nucleotídeos de Purina/metabolismo; Piridinas/farmacocinética; Pirróis/farmacocinética

Palavras-chave

Amide bridge; Classical antifolates; Folate receptor; Pyrrolo[2,3-d]pyrimidines; Selective uptake

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piridinas / Pirróis / Antagonistas do Ácido Fólico / Antineoplásicos Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article

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