Design, synthesis and biological evaluation of novel pyrrolo[2,3-d]pyrimidine as tumor-targeting agents with selectivity for tumor uptake by high affinity folate receptors over the reduced folate carrier.

Golani, Lalit K; Islam, Farhana; O'Connor, Carrie; Dekhne, Aamod S; Hou, Zhanjun; Matherly, Larry H; Gangjee, Aleem

Golani, Lalit K; Islam, Farhana; O'Connor, Carrie; Dekhne, Aamod S; Hou, Zhanjun; Matherly, Larry H; Gangjee, Aleem.

Afiliación

Golani LK; Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States. Electronic address: lalit2510@gmail.com.
Islam F; 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.
Dekhne AS; 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 East Canfield, 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 East Canfield, Detr
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 ; 28(12): 115544, 2020 06 15.

Article en En | MEDLINE | ID: mdl-32503687

Asunto(s)

Antineoplásicos/síntesis química; Diseño de Fármacos; Receptor 1 de Folato/metabolismo; Receptor 2 de Folato/metabolismo; Ácido Fólico/metabolismo; Pirimidinas/química; Pirroles/química; Animales; Antineoplásicos/metabolismo; Antineoplásicos/farmacología; Sitios de Unión; Células CHO; Dominio Catalítico; Línea Celular Tumoral; Cricetinae; Cricetulus; Receptor 1 de Folato/química; Receptor 1 de Folato/genética; Receptor 2 de Folato/química; Receptor 2 de Folato/genética; Ácido Fólico/química; Antagonistas del Ácido Fólico/síntesis química; Antagonistas del Ácido Fólico/metabolismo; Antagonistas del Ácido Fólico/farmacología; Humanos; Simulación del Acoplamiento Molecular; Fosforribosilglicinamida-Formiltransferasa/química; Fosforribosilglicinamida-Formiltransferasa/metabolismo; Pirimidinas/metabolismo; Pirimidinas/farmacología; Pirroles/metabolismo; Pirroles/farmacología; Relación Estructura-Actividad

Palabras clave

Folate receptor; Heteroatom bridge; Pyrrolo[2,3-d]pyrimidine; Reduced folate carrier; Selective uptake

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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Pirimidinas / Pirroles / Diseño de Fármacos / Receptor 1 de Folato / Receptor 2 de Folato / Ácido Fólico / Antineoplásicos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article

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