期刊
ARCHIV DER PHARMAZIE
卷 346, 期 1, 页码 34-43出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201200220
关键词
Antiproliferative activity; A375 melanoma cells; Bischromone derivatives
资金
- Medical University in Lodz, Poland [503/3-011-03/503-01, 503/1-156-01/503-01]
- Polpharma Science Foundation
The synthesis of new bischromone derivatives (4ac and 5ac) as potential anticancer drugs is described. The difference in the reactivity between 4-oxo-4H-chromene-3-carboxylic acid 2 (or its methyl ester 3) and 4-oxo-4H-chromene-3-carbonyl chloride 1 with three different polyamines: 3,3'-diamino-N-methyldipropylamine (a), 1,4-bis(3-aminopropyl)piperazine (b), 4,9-dioxa-1,12-dodecanediamine (c) resulted in the formation of two different groups of products, compounds 4ac and 5ac, designed in agreement with the bisintercalators' structural requirements. The transformation of 4-oxo-4H-chromene-3-carboxylic acid into 2H-chromene-2,4(3H)-diones (5) was confirmed by the NMR and XRD experiments. Compounds 4a and 5a were evaluated in vitro in the highly aggressive melanoma cell line A375. An enhanced induction of apoptosis and cell cycle arrest clearly revealed that compound 5a was more potent than 4a. Compound 5a was also more active in diminishing the adhesive potential of melanoma cells. Current studies support the notion that small changes in the three-dimensional structure of molecules might have a substantial impact on their biological activity.
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