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Zeitschrift für Naturforschung B

A Journal of Chemical Sciences

12 Issues per year

IMPACT FACTOR 2017: 0.757

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Volume 69, Issue 7


Synthesis of New TGX-221 Analogs

Chunjing Liu / Benyi Li
  • Department of Urology, The University of Kansas Medical Center, 3901 Rainbow Bouleward, Kansas City, KS66160, USA
  • Other articles by this author:
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/ Lester Mitscher
Published Online: 2014-06-02 | DOI: https://doi.org/10.5560/znb.2014-4081

TGX-221 is a potent phosphoinositide 3-kinase (PI3K)β inhibitor that has great therapeutic potential to treat prostate cancer. Chemical modification of TGX-221 at positions 2 and 9 was made. Five new TGX-221 analogs with different heterocyclic substituents of morpholine, 1-methylpiperazine, aniline, and thiazole-2-amine at positions 2 and 9 were synthesized. Parallel synthetic methods were employed in SN2 replacement reactions at positions 2 and 9 of TGX-221.

Graphical Abstract

Synthesis of New TGX-221 Analogs

Synthesis of New TGX-221 Analogs

Keywords: TGX-221; Heterocyclic Substituent; Parallel Synthesis; SN2 Reaction; Microwave Reaction

About the article

Received: 2014-03-31

Published Online: 2014-06-02

Published in Print: 2014-07-01

Citation Information: Zeitschrift für Naturforschung B, Volume 69, Issue 7, Pages 817–822, ISSN (Online) 1865-7117, ISSN (Print) 0932-0776, DOI: https://doi.org/10.5560/znb.2014-4081.

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© 1946 – 2014: Verlag der Zeitschrift für Naturforschung.

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