Selective Synthesis and Reactions of 6-Substituted- 2-β-galactosyl-1,2,4-triazines of Potential Anticancer Activity

Abstract

Selective synthesis and reactions of different 6-substituted-2-β-D-galactosyl-3-thioxo-2,3-dihydro-1,2,4-triazin-5(4H)-ones using the developed amino or aryl protecting group strategy were investigated. Primary human anticancer screening of twelve selected compounds (in vitro) resulted in an active compound against both MCF7 (Breast) and SF-268(CNS) cell lines.

Key Words:

• Synthesis
• 1,2,4-Triazines
• Galactosides
• Anticancer activity

Acknowledgments

The authors are very grateful to Dr. V. L. Narayanan and Dr. Edward Sausvile, National Cancer Institute/National Institutes of Health, Bethesda, Maryland, USA, for their valuable anticancer testing.

Notes

Compound 5a is an illustrative example that shows how J values including coupling protons assign different CH′ protons of the sugar moiety.