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1.
Toxins (Basel) ; 7(12): 5408-16, 2015 Dec 11.
Artigo em Inglês | MEDLINE | ID: mdl-26690479

RESUMO

Due to its tropical location, chains of mountains, inter-Andean valleys, Amazon basin area, eastern plains and shores on both the Atlantic and Pacific Oceans, Colombia has many ecosystems and the second largest plant biodiversity in the world. Many plant species, both native and naturalized, are currently recognized as toxic for both animals and humans, and some of them are known to cause their toxic effects due to their alkaloid content. Among these, there are plants containing the hepatotoxic pyrrolizidine alkaloids, neurotoxins such as the indolizidine alkaloid swainsonine and the piperidine alkaloids coniine and γ-coniceine and tropane alkaloids. Unfortunately, the research in toxic plants in Colombia is not nearly proportional to its plant biodiversity and the scientific information available is only very scarce. The present review aims at summarizing the scarce information about plant alkaloid toxicosis in animals and humans in Colombia.


Assuntos
Alcaloides/toxicidade , Plantas Tóxicas/toxicidade , Animais , Colômbia , Humanos , Indolizidinas/toxicidade , Piperidinas/toxicidade
2.
Bioorg Med Chem ; 22(15): 4001-9, 2014 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-24997575

RESUMO

The field of small-molecule inhibitors of protein-protein interactions is rapidly advancing and the specific area of inhibitors of the p53/MDM2 interaction is a prime example. Several groups have published on this topic and multiple compounds are in various stages of clinical development. Building on the strength of the discovery of RG7112, a Nutlin imidazoline-based compound, and RG7388, a pyrrolidine-based compound, we have developed additional scaffolds that provide opportunities for future development. Here, we report the discovery and optimization of a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitors, culminating in RO8994.


Assuntos
Indóis/química , Indolizidinas/química , Proteínas Proto-Oncogênicas c-mdm2/antagonistas & inibidores , Compostos de Espiro/química , Apoptose/efeitos dos fármacos , Sítios de Ligação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Humanos , Imidazolinas/química , Indóis/uso terapêutico , Indóis/toxicidade , Indolizidinas/uso terapêutico , Indolizidinas/toxicidade , Simulação de Dinâmica Molecular , Neoplasias/tratamento farmacológico , Ligação Proteica , Estrutura Terciária de Proteína , Proteínas Proto-Oncogênicas c-mdm2/metabolismo , Pirrolidinas/química , Compostos de Espiro/uso terapêutico , Compostos de Espiro/toxicidade , Proteína Supressora de Tumor p53/antagonistas & inibidores , Proteína Supressora de Tumor p53/metabolismo , para-Aminobenzoatos/química
3.
Bioorg Med Chem Lett ; 21(1): 342-5, 2011 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-21126872

RESUMO

The asymmetric total synthesis of the strongly cytotoxic phenanthroindolizidine alkaloid 3 was achieved. Using the same route, various derivatives were also synthesized. Cytotoxicity of those synthetic compounds was evaluated and compounds 19, 23, and 27 demonstrated potent cytotoxicities similar to that of 3. The in vivo antitumor efficacy of selected compounds was also evaluated and 23 demonstrated moderate antitumor efficacy.


Assuntos
Alcaloides/química , Antineoplásicos/síntese química , Indolizidinas/síntese química , Indolizinas/química , Fenantrolinas/síntese química , Alcaloides/uso terapêutico , Alcaloides/toxicidade , Antineoplásicos/uso terapêutico , Antineoplásicos/toxicidade , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Indolizidinas/uso terapêutico , Indolizidinas/toxicidade , Neoplasias/tratamento farmacológico , Fenantrolinas/química , Fenantrolinas/uso terapêutico , Fenantrolinas/toxicidade , Relação Estrutura-Atividade
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