沃特曼宁
化学
激酶
圆周率
细胞毒性
选择性
立体化学
酶
生物化学
磷脂酰肌醇
体外
催化作用
作者
Peter Wipf,Daniel J. Minion,Robert J. Halter,Margareta Berggren,Caroline B. Ho,Gary G. Chiang,Lynn Kirkpatrick,Robert T. Abraham,Garth Powis
摘要
A series of viridin analogs was prepared from wortmannin by nucleophilic ring opening at C(20) and evaluated against the signaling kinases PI-3-kinase and mTOR. Several subnanomolar enzyme inhibitors with orders of magnitude selectivity for PI-3-kinase and strong cytotoxic activity against four cancer cell lines were identified. Among the ten most promising derivatives, six demonstrated lower liver toxicity and greater promise for inhibition of tumor cell growth than the lead structure wortmannin.
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