Trilobolide-steroid hybrids: Synthesis, cytotoxic and antimycobacterial activity

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• 作者：Michal Jurá ; &scaron ; ek^a ; Petr Džubá ; k^b ; ^{dzubakp@gmail.com} ; Silvie Rimpelová ; ^a ; David Sedlá ; k^c ; Petr Konečný ; ^b ; Ivo Frydrych^b ; Soňa Gurská ; ^b ; Mariá ; n Hajdú ; ch^b ; Kateřina Bogdanová ; ^b ; Milan Kolá ; ř^b ; Tomá ; &scaron ; Mü ; ller^c ; Eva Kmoní ; čková ; ^d ; ^e ; Tomá ; &scaron ; Ruml^a ; Juraj Harmatha^f ; Pavel B. Dra&scaron ; ar^a ; ^{pavel.drasar@vscht.cz}
• 关键词：Trilobolide ; Steroids ; Click chemistry ; Cytotoxicity ; SAR ; Steroid receptor
• 刊名：Steroids
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：117
• 期：Complete
• 页码：97-104
• 全文大小：2477 K
• 卷排序：117

文摘

Five trilobolide-steroid hybrids were synthesized using CuAAC approach. Cytotoxicity was tested on a 12 cancer and 3 non-cancerous cell lines. The most cytotoxic compounds were tested for cell-cycle analysis on CCRF-CEM line. The potency on androgen (AR) and estrogen (α,β-ER) receptors was examined. Impact on cell morphology was studied by live-cell microscopy. Compounds were tested against 8 sensitive and multiresistant bacterial and Candida strains.