Stefane Bogdan, Brozic Petra, Vehovc Matej, Rizner Tea Lanisnik, Gobec Stanislav
Faculty of Chemistry and Chemical Technology, University of Ljubljana, Askerceva 5, 1000 Ljubljana, Slovenia.
Eur J Med Chem. 2009 Jun;44(6):2563-71. doi: 10.1016/j.ejmech.2009.01.028. Epub 2009 Feb 5.
A series of cyclopentane derivatives was synthesized and evaluated for inhibition of the steroid metabolizing enzymes AKR1C1 and AKR1C3. Selective inhibitors that are active in the low micromolar range were identified. These compounds represent promising starting points in the development of new anticancer agents for the treatment of hormone-dependent forms of cancer and other diseases where AKR1C1 and AKR1C3 are involved.
合成了一系列环戊烷衍生物，并对其抑制类固醇代谢酶AKR1C1和AKR1C3的能力进行了评估。鉴定出了在低微摩尔范围内具有活性的选择性抑制剂。这些化合物是开发新型抗癌药物的有希望的起点，可用于治疗激素依赖性癌症以及其他涉及AKR1C1和AKR1C3的疾病。
