Modular Synthesis and Antiproliferative Activity of New Dihydro-1H-pyrazolo[1,3-b]pyridine Embelin Derivatives

Autor:	Borja Guerra, Pedro Martín-Acosta, Leandro Fernández-Pérez, Ángel Amesty, Miguel Guerra-Rodríguez, Ana Estévez-Braun
Rok vydání:	2021
Předmět:	antiproliferative activity embelin multicomponent reaction Chemistry Stereochemistry In silico Acute erythroid leukemia Pharmaceutical Science Myeloid leukemia medicine.disease Article RS1-441 chemistry.chemical_compound Pharmacy and materia medica SKBR3 Drug Discovery Pyridine Vero cell medicine Medicine Molecular Medicine Cytotoxicity SAR ADME
Zdroj:	Pharmaceuticals, Vol 14, Iss 1026, p 1026 (2021) Pharmaceuticals Volume 14 Issue 10
ISSN:	1424-8247
DOI:	10.3390/ph14101026
Popis:	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.
Databáze:	OpenAIRE
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