聚乙炔苷衍生物的合成、抗肿瘤和抗病毒评估。

IF 2.9 3区化学 Q1 CHEMISTRY, ORGANIC Organic & Biomolecular Chemistry Pub Date : 2024-11-21 DOI:10.1039/d4ob01595a

Jonh A M Santos, Robrigo R A Caiana, Cláudia L A Almeida, Daniel C Pimenta, Kleber J S Farias, Renato F de Almeida Júnior, Paula R L Machado, Paulo H Menezes, Juliano C R Freitas

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引用次数: 0

摘要

我们合成了一系列新型聚乙炔苷（PAGs）衍生物，并评估了它们的抗增殖和抗病毒特性。以D-(+)-葡萄糖五乙酸酯为前体（一种市场上可买到的低成本起始原料），尝试了三种不同的策略合成新的PAGs，仅用了三个步骤就以较高的总产率获得了所需的化合物。合成的 PAG 在 68-878 μM 浓度范围内具有抗肿瘤活性，在 71-794 μM 浓度范围内具有抗病毒活性。本文还讨论了一些初步的结构-活性关系。

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Synthesis, and antitumoral and antiviral evaluation of polyacetylene glycoside derivatives.

A series of novel derivatives of Poliacetylene Glycosides (PAGs) were synthesized, and their antiproliferative and antiviral properties were evaluated. Starting from D-(+)-glucose pentaacetate as a precursor, a commercially available and low-cost starting material, three different strategies were attempted to synthesize the new PAGs, and the desired compounds were obtained in high overall yields after only three steps. The synthesized PAGs exhibited antitumoral activity in concentrations ranging from 68-878 μM and antiviral activities in concentrations ranging from 71-794 μM. Some preliminary structure-activity relationships are also discussed.

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