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
Received: 2014-3-31
Published Online: 2014-6-2
Published in Print: 2014-7-1
© 1946 – 2014: Verlag der Zeitschrift für Naturforschung
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Keywords for this article
TGX-221;
Heterocyclic Substituent;
Parallel Synthesis;
SN2 Reaction;
Microwave Reaction
Articles in the same Issue
- Synthesis, Structure and Thermal Decomposition of a New Iodine Inclusion Compound in the 2,2-Dimethylpropane-1,3-diamine/HI/I2 System
- Rapid Microwave Synthesis and Structural Phase Diagram of LnxY1−xMnO3
- Gold-Tin Ordering in SrAu2Sn2
- The Stannides EuPd2Sn2, EuPt2Sn2, EuAu2Sn2, and Eu5.4Sn5.6 – Structure and Magnetic Properties
- Line-Shape Analyses of Solid-state 17O NMR Spectra for Hexagonal Ice
- A Novel Alkali-Metal Hydrido-tris(pyrazolyl)borate (Tp*) Complex. Isolation and Crystal Structure of [(Me2CO)3(NaTp*)2]
- Synthesis and Structure of an Aluminum Bis(3-chloropentanedionate) Isopropoxide: [Al(μ-OiPr)(3-Clacac)2]2
- Carbon-modified MgH2: Experimental and ab-initio Investigations
- Synthesis and Antitumor Activity of Some N2-(Thien-3-yl)amidrazones
- Synthesis of New TGX-221 Analogs
- Crystal Structure Explains Crystal Habit for the Antiviral Drug Rimantadine Hydrochloride
- The Reaction of Cyanamidium Salts with Ylidenecyanamide Derivatives
- Iridoid Glycosides from Lagotis alutacea
- Solid-state and Calculated Electronic Structure of 4-Acetylpyrazole