College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon 406-779, Republic of Korea.
College of Pharmacy, Korea University, Sejong 339-700, Republic of Korea.
Bioorg Med Chem Lett. 2014 May 1;24(9):2062-5. doi: 10.1016/j.bmcl.2014.03.047. Epub 2014 Mar 25.
A xanthone-derived natural product, α-mangostin is isolated from various parts of the mangosteen, Garcinia mangostana L. (Clusiaceae), a well-known tropical fruit. Novel xanthone derivatives based on α-mangostin were synthesized and evaluated as anti-cancer agents by cytotoxicity activity screening using 5 human cancer cell lines. Some of these analogs had potent to moderate inhibitory activities. The structure-activity relationship studies revealed that phenol groups on C3 and C6 are critical to anti-proliferative activity and C4 modification is capable to improve both anti-cancer activity and drug-like properties. Our findings provide new possibilities for further explorations to improve potency.
从藤黄科藤黄属植物山竹的各个部位中分离得到一种桔酮类天然产物，即 α-倒捻子素。新型桔酮衍生物基于 α-倒捻子素合成，并通过使用 5 个人类癌细胞系进行细胞毒性活性筛选来评估其作为抗癌剂的活性。其中一些类似物具有较强至中等的抑制活性。构效关系研究表明，C3 和 C6 位上的酚基对增殖抑制活性至关重要，而 C4 位的修饰能够提高抗癌活性和类药性。我们的研究结果为进一步提高其活性提供了新的可能性。
