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Z. Naturforsch. 2014,
69b, 817 – 822
doi:10.5560/ZNB.2014-4081
Synthesis of New TGX-221 Analogs
1 Higuchi Biosciences Center, The University of Kansas, Lawrence, KS66045, USA
2 Department of Urology, The University of Kansas Medical Center, 3901 Rainbow Bouleward, Kansas City, KS66160, USA
3 Department of Medicinal Chemistry, The University of Kansas, Lawrence, KS66045, USA
Reprint requests to Dr. Chunjing Liu. E-mail:
cjliu2@gmail.com
Received March 31, 2014 / published online July 8, 2014
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.
Key words: TGX-221, Heterocyclic Substituent, Parallel Synthesis, SN2 Reaction, Microwave Reaction