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Title: | Modular Synthesis and Antiproliferative Activity of New Dihydro-1H-pyrazolo[1,3-b]pyridine Embelin Derivatives | Authors: | Martín-Acosta, Pedro Amesty, Ángel Guerra Rodríguez, Miguel Alfonso Guerra Hernández, Carlos Borja Fernández Pérez, Leandro Fco Estévez-Braun, Ana |
UNESCO Clasification: | 32 Ciencias médicas 3209 Farmacología 2306 Química orgánica |
Keywords: | Multicomponent reaction Embelin Antiproliferative activity SAR |
Issue Date: | 2021 | Project: | Cribado Farmacológico de Librerías Químicas y Desarrollo Preclínico de Nuevas Entidades Moduladoras de Los Oncogenes Stat3/5 y Yap1, y Del Receptor de Estrógenos (Serm) Aplicación de Una Plataforma de Bioensayos en El Cribado de Bibliotecas Químicas Inspiradas en la Biodiversidad: Identificación y Desarrollo de Moléculas Con Interés Biomédico en Oncología. |
Journal: | Pharmaceuticals | Abstract: | A set of new dihydro-1H-pyrazolo[1,3-b]pyridine and pyrazolo[1,3-b]pyridine embelin derivatives was synthesized through a multicomponent reaction from natural embelin, 3-substituted-5-aminopyrazoles and aldehydes. The synthesized compounds were evaluated against three hematologic tumor cell lines, HEL (acute erythroid leukemia), K-562 (chronic myeloid leukemia) and HL-60 (acute myeloid leukemia), and five breast cancer cell lines (SKBR3, MCF-7, MDA-MB-231, BT-549, HS-578T). The primate non-malignant kidney Vero cell line was used as the control of cytotoxicity. From the obtained results, some structure–activity relationships were outlined. Furthermore, in silico prediction of physicochemical properties and ADME parameters were determined for the derivatives with the best antiproliferative values | URI: | http://hdl.handle.net/10553/112279 | ISSN: | 1424-8247 | DOI: | 10.3390/ph14101026 | Source: | Pharmaceuticals [ISSN 1424-8247], v. 14(10), 1026 |
Appears in Collections: | Artículos |
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