Synthesis, and QSAR analysis of anti-oncological active spiro-alkaloids.
Org Biomol Chem
; 13(6): 1741-53, 2015 Feb 14.
Article
em En
| MEDLINE
| ID: mdl-25502495
ABSTRACT
QSAR study describes the anti-neoplastic spiro-alkaloids with relevant molecular descriptors using CODESSA III software. The dispiro[3H-indole-3,2'-pyrrolidine-3',3"-piperidines] 24-48 were synthesized via [3 + 2]-cycloaddition reaction of azomethine ylides, (generated in situ via decarboxylative condensation of isatins 21-23 with sarcosine) and 3E,5E-1-alkyl-3,5-bis(arylmethylidene)-4-piperidones 10-20. Some of the synthesized analogues exhibited promising antitumor properties against HELA (cervical), HEPG2 (liver), T-47D, MCF7 (breast), and HCT116 (colon) human tumor cell lines, demonstrating activity close to or even better than the standard Doxorubicin, based on in vitro Sulfo-Rhodamine-B bio-assay.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos de Espiro
/
Relação Quantitativa Estrutura-Atividade
/
Alcaloides
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article