AHMAD FATIH JAUHARI (2015) SINTESIS DAN UJI AKTIVITAS SITOTOKSIK ASAM 10-N-(BENZOIL) FOLAT PADA SEL HELA. Skripsi thesis, UNIVERSITAS AIRLANGGA.

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Abstract

In Indonesia, each year approximately 15,000 new cases of cervical cancer and 7,500 of them lead to death. In cancer cells was found that excess folic acid needs. Have been many analog of folic acid (antifolate) is used as the analog cancer chemotherapy but still have considerable side effects. So it is necessary to modify the folic acid molecule to produce another analog that is expected to provide an optimal activity but have low toxicity. Folic acid modification begins with drafting a compound where folic acid is added the groups which have lipophilic properties, electronic and steric certain. Then tested in silico to predict bond strength analogous to receptors. Then do the synthesis of these compounds with acylation method and the its analog results tested the activity with in vitro assays in HeLa cells that compared to the positive control (methotrexate) with MTT assay method. Results from in silico test shows modified compounds have lower scores rerank (potent). Results compound from synthesis is 10-N- (benzoyl)folic acid with 60% yield and proved by TLC and 1H-NMR spectrophotometric test. Then results compound from synthesis tested with MTT assay test against HeLa cell culture that compared with methotrexate at a level of 5000 ppm until 10 ppm. The result from MTT assay test can not be analyzed because the method does not show the good hindrance between 10-N- (benzoyl) folic acid and methotrexate. This research resulted in 10-N- (benzoyl)folic acid as antifolate.

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