化学
丝氨酸
苏氨酸
蛋白磷酸酶2
卵巢癌
生物化学
癌症研究
磷酸酶
磷酸化
癌症
卵巢癌
内科学
生物
医学
作者
Marieke van der Hart,A. Richard Chamberlin,Cecilia Walkom,Jennette A. Sakoff,Adam McCluskey
标识
DOI:10.1016/j.bmcl.2004.01.093
摘要
Fourteen modified norcantharidin analogues have been synthesised and screened for their ability to inhibit the serine/threonine protein phosphatases 1 and 2A. The most potent compounds found were 10 (PP1 IC50=13±5 μM; PP2A IC50=7±3 μM) and 16 (PP1 IC50=18±8 μM; PP2A IC50=3.2±0.4 μM). Overall, only analogues possessing at least one acidic residue at the former anhydride warhead displayed any PP1 or PP2A inhibitory action. The ability of these analogues to inhibit PP1 and PP2A correlates well with their observed anti-cancer activity against a panel of five cancer cell lines: A2780 (human ovarian carcinoma), G401 (human kidney carcinoma), HT29 (human colorectal carcinoma), H460 (human lung carcinoma) and L1210 (murine leukemia).
科研通智能强力驱动
Strongly Powered by AbleSci AI