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Chen Z.,Shanghai Institute of Pharmaceutical Industry | Li J.,Shanghai Institute of Pharmaceutical Industry | Lin H.,Shanghai Institute of Pharmaceutical Industry | Shao L.,Shanghai Institute of Pharmaceutical Industry | And 4 more authors.
Journal of Bioscience and Bioengineering | Year: 2013

The biotransformation of 14-deoxy-14-methylenetriptolide by Neurospora crassa CGMCC AS 3.1604 to produce a new hydroxylation derivative was studied. The structure of this novel compound was determined using spectral data. This biotransformation using whole cells conditioned for 4 days transformed approximately 65% (mol ratio) of the substrate into the compound (5R)-5-hydroxy-14-deoxy-14-methylenetriptolide. © 2013 The Society for Biotechnology, Japan. Source

Cheng J.,Shanghai Huilun Life science and Technology Co. | Qin J.,Shanghai Huilun Life science and Technology Co. | Guo S.,Shanghai Huilun Life science and Technology Co. | Qiu H.,Shanghai Huilun Life science and Technology Co. | Zhong Y.,Shanghai Huilun Life science and Technology Co.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

Phenyl imidazolidin-2-one was introduced as the linker for novel HDAC inhibitors. A focused library of 20 compounds was designed and synthesized, among which eight compounds showed equivalent or higher potencies against HDAC1 as compared to vorinostat. In vitro antitumor activity assays in HCT-116, PC-3 and HL-60 cancer cells revealed six compounds with potent antitumor activities, and compound 1o showed 6- to 9-fold higher potencies compared to vorinostat. In an HCT-116 nude mice xenograft model, compound 1o displayed significant antitumor activity in both continuous and intermittent dosing schedules. © 2014 Elsevier Ltd. All rights reserved. Source

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