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

Overview

Journal Pharmaceuticals (Basel)

Publisher MDPI

Specialty Chemistry

Date 2021 Oct 23

PMID 34681250

Citations 4

Authors

Pedro Martin-Acosta

Angel Amesty

Miguel Guerra-Rodriguez

Borja Guerra

Leandro Fernandez-Perez

Ana Estevez-Braun

Affiliations

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Abstract

A set of new dihydro-1-pyrazolo[1,3-]pyridine and pyrazolo[1,3-]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.

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