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1.
Molecules ; 25(1)2019 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-31892146

RESUMO

Cancer is a disease that involves impaired genome stability with a high mortality index globally. Since its discovery, many have searched for effective treatment, assessing different molecules for their anticancer activity. One of the most studied sources for anticancer therapy is natural compounds and their derivates, like alkaloids, which are organic molecules containing nitrogen atoms in their structure. Among them, oxoisoaporphine and sampangine compounds are receiving increased attention due to their potential anticancer effects. Boldine has also been tested as an anticancer molecule. Boldine is the primary alkaloid extract from boldo, an endemic tree in Chile. These compounds and their derivatives have unique structural properties that potentially have an anticancer mechanism. Different studies showed that this molecule can target cancer cells through several mechanisms, including reactive oxygen species generation, DNA binding, and telomerase enzyme inhibition. In this review, we summarize the state-of-art research related to oxoisoaporphine, sampangine, and boldine, with emphasis on their structural characteristics and the relationship between structure, activity, methods of extraction or synthesis, and anticancer mechanism. With an effective cancer therapy still lacking, these three compounds are good candidates for new anticancer research.


Assuntos
Alcaloides , Antineoplásicos Fitogênicos , Aporfinas , Inibidores Enzimáticos , Compostos Heterocíclicos de 4 ou mais Anéis , Naftiridinas , Neoplasias/tratamento farmacológico , Alcaloides/química , Alcaloides/uso terapêutico , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/uso terapêutico , Aporfinas/química , Aporfinas/uso terapêutico , Inibidores Enzimáticos/química , Inibidores Enzimáticos/uso terapêutico , Compostos Heterocíclicos de 4 ou mais Anéis/química , Compostos Heterocíclicos de 4 ou mais Anéis/uso terapêutico , Humanos , Naftiridinas/química , Naftiridinas/uso terapêutico , Proteínas de Neoplasias/antagonistas & inibidores , Proteínas de Neoplasias/metabolismo , Neoplasias/metabolismo , Neoplasias/patologia , Telomerase/antagonistas & inibidores , Telomerase/metabolismo
2.
Arch Pharm (Weinheim) ; 350(1)2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27981607

RESUMO

A series of novel 3-indolylpropyl derivatives was synthesized and evaluated for their binding affinities at the serotonin-1A receptor subtype (5-HT1A R) and the 5-HT transporter (SERT). Compounds 11b and 14b exhibited the highest affinities at the 5-HT1A R (Ki = 43 and 56 nM), whereas compounds 11c and 14a were the most potent analogs at the SERT (Ki = 34 and 17 nM). On the other hand, compounds 14b and 11d showed potent activity at both targets, displaying a profile that makes them promising leads for the search for novel potent ligands with a dual mechanism of action. Molecular docking studies in all the compounds unveiled relevant drug-target interactions, which allowed rationalizing the observed affinities.


Assuntos
Indóis/síntese química , Indóis/farmacologia , Simulação de Acoplamento Molecular , Receptor 5-HT1A de Serotonina/metabolismo , Serotoninérgicos/síntese química , Serotoninérgicos/farmacologia , Proteínas da Membrana Plasmática de Transporte de Serotonina/metabolismo , Antidepressivos/síntese química , Antidepressivos/farmacologia , Relação Dose-Resposta a Droga , Humanos , Indóis/química , Estrutura Molecular , Serotoninérgicos/química , Relação Estrutura-Atividade
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