Literature DB >> 19616947

Discovery of CYT997: a structurally novel orally active microtubule targeting agent.

Christopher J Burns1, Michael F Harte, Xianyong Bu, Emmanuelle Fantino, Max Joffe, Harrison Sikanyika, Stephen Su, C Elisabet Tranberg, Neil Wilson, Susan A Charman, David M Shackleford, Andrew F Wilks.   

Abstract

CYT997 was discovered as a potent tubulin polymerization inhibitor possessing potent cytotoxic activity against a range of cancer cells. Details of SAR studies, pharmacokinetic investigations and synthesis of compounds leading to the discovery of CYT997 are reported.

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Year:  2009        PMID: 19616947     DOI: 10.1016/j.bmcl.2009.06.079

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

1.  Autophagy blockade sensitizes human head and neck squamous cell carcinoma towards CYT997 through enhancing excessively high reactive oxygen species-induced apoptosis.

Authors:  Lixia Gao; Xiangdong Zhao; Liwei Lang; Chloe Shay; W Andrew Yeudall; Yong Teng
Journal:  J Mol Med (Berl)       Date:  2018-07-18       Impact factor: 4.599

2.  CYT997 causes apoptosis in human multiple myeloma.

Authors:  Katherine Monaghan; Tiffany Khong; Gregg Smith; Andrew Spencer
Journal:  Invest New Drugs       Date:  2009-11-12       Impact factor: 3.850

3.  Phase I trial of CYT997, a novel cytotoxic and vascular-disrupting agent.

Authors:  J D Lickliter; A B Francesconi; G Smith; M Burge; A Coulthard; S Rose; M Griffin; R Milne; J McCarron; T Yeadon; A Wilks; A Cubitt; D K Wyld; P A Vasey
Journal:  Br J Cancer       Date:  2010-08-24       Impact factor: 7.640

4.  Augmentation of the anticancer activity of CYT997 in human prostate cancer by inhibiting Src activity.

Authors:  Yong Teng; Yafei Cai; Wenhu Pi; Lixia Gao; Chloe Shay
Journal:  J Hematol Oncol       Date:  2017-06-12       Impact factor: 17.388

5.  Mitochondrial ROS accumulation inhibiting JAK2/STAT3 pathway is a critical modulator of CYT997-induced autophagy and apoptosis in gastric cancer.

Authors:  Ya Cao; Jinglong Wang; Hua Tian; Guo-Hui Fu
Journal:  J Exp Clin Cancer Res       Date:  2020-06-23

6.  The microtubule depolymerizing agent CYT997 effectively kills acute myeloid leukemia cells via activation of caspases and inhibition of PI3K/Akt/mTOR pathway proteins.

Authors:  Xiaohui Chen; Chunmei Yang; Yanhua Xu; Hui Zhou; Hui Liu; Wenbin Qian
Journal:  Exp Ther Med       Date:  2013-06-14       Impact factor: 2.447

7.  Intracellular reduction in ATP levels contributes to CYT997-induced suppression of metastasis of head and neck squamous carcinoma.

Authors:  Xiangdong Zhao; Liwei Lang; Leilei He; Lixia Gao; David Chyan; Yuanping Xiong; Honglin Li; Hong Peng; Yong Teng
Journal:  J Cell Mol Med       Date:  2018-11-18       Impact factor: 5.310

8.  CYT997(Lexibulin) induces apoptosis and autophagy through the activation of mutually reinforced ER stress and ROS in osteosarcoma.

Authors:  Zongyi Wang; Fei Yin; Jing Xu; Tao Zhang; Gangyang Wang; Ming Mao; Zhuoying Wang; Wei Sun; Jing Han; Mengkai Yang; Yafei Jiang; Yingqi Hua; Zhengdong Cai
Journal:  J Exp Clin Cancer Res       Date:  2019-01-31
  8 in total

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