Synthesis and biological evaluation of novel benzo[b]xanthone derivatives as potential antitumor agents

Abstract

Nine novel aminoalkoxy substituted benzoxanthones (3a-3i) were synthesized. Their antitumor activities were evaluated in five human solid tumor cell lines including Hep-G2, BEL-7402, HeLa, MGC-803 and CNE by MTT method. The results showed that most of the compounds displayed moderate to good inhibitory activities on the tested cancer cell lines in vitro, among them compounds 3a and 3h showed higher antitumor activity than other tested compounds against most cell lines. The influence of two kinds of structural factors including the terminal amino group and length of carbon spacers on the anticancer activities were explored to discuss the preliminary structure-activity relationships

The Effect of Mangosteen (Garcinia Mangostana) Pericarp Extract on Retinoblastoma Cell Culture Proliferation

“…In the largest doses of 100 µg/ml 25% of the SK-MEL-28 cells dead. 7,13,14 The limitation of this research is limited in the previous literature review. From some literature also obtained various sources stating differences in dosage and the incubation period.…”

“…As for the antitumor activity xanthones among other inhibit cell cycle, suppression of tumor cell proliferation, induction of apoptosis and differentiation, reduce inflammation and inhibits adhesion, invasion and metastasis of tumors. 7,9 The aim of this study to determine the effect of mangosteen pericarp extract (Garcinia mangostana) on retinoblastoma cell culture proliferation. Cell culture will be exposed with the mangosteen pericarp extract in different doses of 10 µg/ml, 20 µg/ml, and 40 µg/ml and incubated for 48 hours.…”

“…Most of these materials have good tumor inhibition activity. 4,5,6,7 In this study, mangosteen pericarp extracts with various doses exposed to retinoblastoma culture cells and then observed using MTT Proliferation Assay to see the effect of mangosteen pericarp extracts (Garcinia mangostana) on retinoblastoma cultured cells proliferation.…”

Recent advances in the synthesis of xanthones and azaxanthones

“…The classical Grover, Shah and Shah method 95,96 constitutes a suitable approach for the synthesis of hydroxyxanthones from easily available salicylic acid derivatives and phenols heated along with zinc chloride in phosphoryl chloride. 33,39,43,49,51,60,65,[97][98][99][100][101][102][103][104] For the reaction to proceed directly to the desired xanthone, the 2,2′-dihydroxybenzophenone intermediate must contain an additional hydroxyl moiety ortho to the carbonyl group. Usually phloroglucinol is used in order to overcome this limitation; however, when other phenol derivatives like resorcinol are used, the synthetic pathway stops at the benzophenone form.…”

“…In the last decade, both natural and synthetic xanthones have been reported with diverse biological and pharmacological properties, 5,6,8,16 including antibacterial, 8,17-27 antifungal, 8,17,20,21,[28][29][30] antiviral, 31 antioxidant, [32][33][34][35][36][37] antiobesity, 38 anti-inflammatory, 5,17,[39][40][41] anticoagulant, 42 and antitumour. 36,[43][44][45][46][47][48][49][50][51][52][53][54][55][56][57][58] Particularly, some xanthones' molecular targets have been disclosed, including clinically important enzymes such as α-glucosidase, [59][60][61][62][63] topoisomerase, 64,…”