Design, synthesis and cytotoxicity of novel hexacyclic saframycin-ecteinascidin analogs.
Org Biomol Chem
; 18(2): 237-249, 2020 01 02.
Article
em En
| MEDLINE
| ID: mdl-31782476
ABSTRACT
Two series of novel hexacyclic skeletons and their thirty-four derivatives were prepared from l-tryptophan and l-DOPA. The cytotoxicities of these compounds were tested against four human cancer cell lines HCT-116, HepG2, BGC-823 and A2780. Compounds with the tetrahydro-ß-carboline moiety in the left-half of the hexacyclic skeleton showed more potent cytotoxicity with IC50 values in the range of 10-7-10-9 M. Compound 20 with the 4-methoxybenzamide side chain showed potent cytotoxicity towards HepG2 with an IC50 value of 1.32 nM. Compounds 29 and 30 with 2-pyridine amide and (2E)-3-(3-thifluoromethyl-phenyl)acrylic amide side chains showed selective cytotoxicity towards A2780 with IC50 values of 1.73 nM and 7 nM, respectively.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Triptofano
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Desenho de Fármacos
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Levodopa
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Citotoxinas
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Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Org Biomol Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2020
Tipo de documento:
Article