Please use this identifier to cite or link to this item: http://hdl.handle.net/10553/112279
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
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