Naslov
Sinteza i ispitivanje citostatskih djelovanja pirimidinskih i purinskih derivata L-askorbinske kiseline
(Synthesis and cytostatic activity evaluation of pyrimidine ad purine derivatives of L-ascorbic acid)

Autori
Wittine, Karlo ; Stipković Babić, Maja ; Kraljević Pavelić Sandra ; Pavelić Krešimir ; Mintas Mladen

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Drugs of the Future / J. Prous, Jr. - Barcelona : Thomson Reuters, 2010

Skup
EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY

Mjesto i datum
Bruxelles, Belgija, 05.09.2010. - 09.09.2010

Vrsta sudjelovanja
Poster

Vrsta recenzije
Nije recenziran

Ključne riječi
pirimidinske baze; L-askorbinska kiselina; citostatska ispitivanja
(pyrimidine bases; L-ascorbic acid; cytostatic activity evaluation)

Sažetak
Nucleoside analogues represent a valuble source that contributes significantly to the arsenal of chemotherapeutic agents against viruses and cancer. The principal aim of this study was to synthesize the new nucleoside congeners in which the sugar ring was substituted with L-ascorbic acid moiety and to evaluate their cytostatic activity potency. L-ascorbic acid itself has been found to be cytotoxic to some human tumor cells, neuroblastoma1, osteosarcoma and retinoblastoma.2 Ascorbic acid and ascorbyl esters have been found to inhibit the proliferation of mouse glioma and human brain tumor cells, glioma (U-373) and glioblastoma (T98G) cells and renal carcinoma cells.3, 4 In addition to that we have demonstrated that pyrimidine and purine derivatives of L-ascorbic acid exert cytostatic activity against malignant cell lines, especially leukemia (IC50 = 0.9 M) and murine mammary carcinoma (IC50 = 1.4 M), as well as other malignant tumor cell lines.5 Based on this finding we have synthesized a series of pyrimidine (1-12) and purine (13-15) derivatives of L-ascorbic acid containing the free hydroxy group (7-9) at C-5 of ethylenic spacer or amino group at C-4 position (5, 6, 10-15) of the lactone ring and evaluated their cytostatic potential.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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