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- Title
Synthesis and Cytotoxic Activity on Human Cancer Cells of Novel Isoquinolinequinone-Amino Acid Derivatives.
- Authors
Valderrama, Jaime A.; Delgado, Virginia; Sepúlveda, Sandra; Benites, Julio; Theoduloz, Cristina; Calderon, Pedro Buc; Muccioli, Giulio G.
- Abstract
A variety of aminoisoquinoline-5,8-quinones bearing α-amino acidsmoietieswere synthesized from 3-methyl-4-methoxycarbonylisoquinoline-5,8-quinone and diverse L- and D-α-amino acid methyl esters. The members of the series were evaluated for their cytotoxic activity against normal and cancer cell lines by using the (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay. From the current investigation, structure-activity relationships demonstrate that the location and structure of the amino acid fragment plays a significant role in the cytotoxic effects. Moderate to high cytotoxic activity was observed and four members, derived from L-alanine, L-leucine, L-phenylalanine, and D-phenylalanine, were selected as promising compounds by their IC50 ranging from 0.5 to 6.25 κM and also by their good selectivity indexes (≥2.24).
- Subjects
CYTOTOXIC T cells; CANCER cell enzymes; QUINONE derivatives; ALANINE; CHEMICAL derivatives; METHYL formate
- Publication
Molecules, 2016, Vol 21, Issue 9, p1199
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules21091199