Synthesis and In vitro Cytotocxic Evaluation of New Quinazolinone Derivatives

The paper presents a simple and efficient synthesis of a series of new quinazolinone derivatives 8a-h. First, the reaction of 5-hydroxyanthranilic acid (6) with acetic anhydride at 160–180oC for 2 h gave the intermediate 7 in high yield. This intermediate was then reacted with amines in acetic acid at 180 oC for 14 h afforded new quinazolinone derivatives 8a-h in 77–92%. Synthesized compounds were structurally confirmed using spectroscopic methods: 1H, 13CNMR and mass spectrum. The bioassay result using three cancer cell lines including SKLU-1 (lung cancer), MCF-7 (breast cancer) and HepG-2 (liver cancer) showed that only compound 8h exhibited significant cytotoxic effect against cancer cell lines tested with IC50 values of 23.09, 27.75 and 30.19 µg/ mL, respectively.

Synthesis of New Zerumbone Hydrazones and Their In vitro Anticancer Activity

Background: A series of new zerumbone hydrazones 5a-f and 9a-f have been synthesized via an in situ procedure in high yields. The structure of synthesized compounds has been confirmed using 1H, 13C NMR and HR-MS. The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Compound 9a showed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Objective: This study aims at developing new zerumbone hydrazones as anticancer agents based on zerumbone, a natural compound wildly growing in Vietnam. Method: A series of new zerumbone hydrazones was designed, synthesized and evaluated for cytotoxicity against three human cancer cell lines, including HepG-2, MCF-7 and SKLu-1 using MTT method. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Conclusion: The research results suggest that some compounds could be considered as a lead for future design of zerumbone hydrazones in which bio-isosteric replacements in ortho position of the phenyl ring could be performed to improve the cytotoxic activity.

NEW QUINAZOLINONE DERIVATIVES: SYTHESIS AND IN VITRO CYTOTOXIC ACTIVITY

The paper presents a simple synthesis of new quinazolinone derivatives 13a-i. Synthesized derivatives were tested for their cytotoxic effect against three cancer cell lines including SKLU-1, MCF-7 and HepG-2. The bioassay result showed that only compound 13e exhibited significant cytotoxic effect against cancer cell lines tested with IC50 values of 9.48, 20.39 and 18.04 µg/ mL, respectively.