| Literature DB >> 25376106 |
Kenzo Arai1, Silvia Buonamici, Betty Chan, Laura Corson, Atsushi Endo, Baudouin Gerard, Ming-Hong Hao, Craig Karr, Kazunobu Kira, Linda Lee, Xiang Liu, Jason T Lowe, Tuoping Luo, Lisa A Marcaurelle, Yoshiharu Mizui, Marta Nevalainen, Morgan Welzel O'Shea, Eun Sun Park, Samantha A Perino, Sudeep Prajapati, Mingde Shan, Peter G Smith, Parcharee Tivitmahaisoon, John Yuan Wang, Markus Warmuth, Kuo-Ming Wu, Lihua Yu, Huiming Zhang, Guo-Zhu Zheng, Gregg F Keaney.
Abstract
A total synthesis of the natural product 6-deoxypladienolide D (1) has been achieved. Two noteworthy attributes of the synthesis are (1) a late-stage allylic oxidation which proceeds with full chemo-, regio-, and diastereoselectivity and (2) the development of a scalable and cost-effective synthetic route to support drug discovery efforts. 6-Deoxypladienolide D (1) demonstrates potent growth inhibition in a mutant SF3B1 cancer cell line, high binding affinity to the SF3b complex, and inhibition of pre-mRNA splicing.Entities:
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Year: 2014 PMID: 25376106 DOI: 10.1021/ol502556c
Source DB: PubMed Journal: Org Lett ISSN: 1523-7052 Impact factor: 6.005