Kumar Rayala Naveen, Lee Seongmin
The Division of Chemical Biology and Medicinal Chemistry, College of Pharmacy, University of Texas at Austin, Austin, TX 78712, USA.
The Division of Chemical Biology and Medicinal Chemistry, College of Pharmacy, University of Texas at Austin, Austin, TX 78712, USA.
Steroids. 2017 Oct;126:74-78. doi: 10.1016/j.steroids.2017.07.008. Epub 2017 Aug 2.
Cephalostatins, ritterazines and their hybrid bis-steroidal pyrazine analogs such as 25-epi-rittereostatin G1 show unusually high potency against a wide range of cancer cell lines. Herein, we report the synthesis and bioactivity of 23-deoxy-25-epi ritterostatin G1, which lacks the 23-hydroxyl group of 25-epi rittereostatin G1. The less oxygenated bis-steroidal pyrazine was ∼50- to 1000-fold less potent than 25-epi ritterostatin G1, highlighting the importance of the 23-hydroxyl group for the antiproliferative activity of the cephalostatin/ritterazine class of drugs.
头霉素、 Ritterazines及其杂合双甾体吡嗪类似物，如25-表-ritterostatin G1，对多种癌细胞系显示出异常高的活性。在此，我们报道了23-脱氧-25-表ritterostatin G1的合成及生物活性，该化合物缺乏25-表ritterostatin G1的23-羟基。含氧量较低的双甾体吡嗪的活性比25-表ritterostatin G1低约50至1000倍，突出了23-羟基对头霉素/Ritterazines类药物抗增殖活性的重要性。
