JOURNAL BROWSE
Search
Advanced SearchSearch Tips
Design, Synthesis and Biological Evaluation of Novel Analogs of Bortezomib
facebook(new window)  Pirnt(new window) E-mail(new window) Excel Download
 Title & Authors
Design, Synthesis and Biological Evaluation of Novel Analogs of Bortezomib
Rao, R. Janaki Rama; Rao, A.K.S. Bhujanga; Swapna, K.; Rani, B. Baby; Kumar, S. Prasanna; Awantika, S.; Murthy, Y.L.N.;
  PDF(new window)
 Abstract
Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.
 Keywords
Bortezomib;human tumor cell lines;A549;PC3; values;
 Language
English
 Cited by
1.
α-Boryl Isocyanides Enable Facile Preparation of Bioactive Boropeptides, Angewandte Chemie International Edition, 2013, 52, 32, 8411  crossref(new windwow)
2.
Peptide-Based Proteasome Inhibitors in Anticancer Drug Design, Medicinal Research Reviews, 2014, 34, 5, 1001  crossref(new windwow)
3.
α-Boryl Isocyanides Enable Facile Preparation of Bioactive Boropeptides, Angewandte Chemie, 2013, 125, 32, 8569  crossref(new windwow)
 References
1.
Goldberg, A. L. Nature. 2003, 426, 895. crossref(new window)

2.
Voges, D.; Zwickl, P.; Baumeister, W. Annu. Rev. Biochem. 1999, 68, 1015. crossref(new window)

3.
Julian Adams.; Yu-Ting Ma.; Ross Stein.; Matthew Baevsky.; Louis Grenier.; Louis Plamondon. U.S. Patent 5780454, 1998.

4.
Orlowski, L. Z.; Zeger, E. L. Expert Opin. Invest. Drugs 2006, 15, 117. crossref(new window)

5.
Dorsey, B. D.; Iqubal, M.; Chatterjee, S.; Menta, E.; Bernardini, R.; Bernareggi, A.; Cassar, P.G.; D'Ansmo, G.; Ferretti, E.; DeMunari, S.; Oliva, A.; Pezzoni, G.; Allievi, C.; Strepponi, I.; Ruggeri, B.; Atori, M.A.; Williams, M.; Mallamo, J.P. J. Med. Chem. 2008, 51, 1068. crossref(new window)

6.
Yongqiang Zhu.; Xin Zhao.; Xinrong Zhu.; Gangwu, Yuejie Li.; Yuheng Ma.; Yunxia Yuan.; Jie Yang.; Yang Hu.; Li Ai.; Qingzhi Gao. J. Med. Chem. 2009, 52, 4192. crossref(new window)

7.
Yongqiang Zhu.; Xinrong Zhu.; Gang Wu.; Yuheng Ma.; Yuejie Li.; Xin Zhao.; Yunxia Yuan.; Jie Yang.; Sen Yu.; Feng Shao.; Rutalo Li.; Yanrong Ke.; Aijun Lu.; Zhenming Liu.; Liangren Zhang. J. Med. Chem. 2010, 53, 1990. crossref(new window)

8.
Yongqiang Zhu.; Shuyang Yao.; Bo Xu, Zemei Ge.; Jingrong Cui.; Tieming Cheng. Bioorg. Med. Chem. Lett. 2009, 6851.

9.
Lowe, J.; Stock, D.; Jap, B.; Baumeister, W.; Huber, R. Science 1995, 268, 533. crossref(new window)

10.
Groll, M.; Ditzal, L.; Lowe, J.; Stock, D.; Bochtler, M. B.; Huber, R. Nature 1997, 386, 463. crossref(new window)

11.
Groll, M.; Huber, R.; Potts, B. C. J. Am. Chem. Soc. 2006, 128, 5136. crossref(new window)

12.
Groll, M.; Brekers, C. R.; Ploegh, H. L.; Ovaa, H. Structure 2006, 14, 451. crossref(new window)

13.
Fraser Pickersgill, John E. Bishop etal. U.S. Patent 0240047A1, 2005.