TY - JOUR
T1 - 5′-Halogenated formycins as inhibitors of 5′-deoxy-5′-methylthioadenosine phosphorylase
T2 - Protection of cells against the growth-inhibitory activity of 5′-halogenated adenosines
AU - Chu, Shih Hsi
AU - Ho, Lynn
AU - Chu, Edward
AU - Savarese, Todd
AU - Chen, Zhi Hao
AU - Rowe, Elizabeth Claflin
AU - Wang Chu, Ming Yu
N1 - Funding Information:
Acknowledgements: This work has been supported by USPHS grants CA 13943, C4 20992, CA 31650, CA 34228, and American Cancer Society Grant CH-266. We are grateful to Drs. Robert E. Parks, Jr. and Paul Calabresi for their encouragement during the course of this investigation. We also thank Dr. James van Epp for assistance with 'H NMR spectra.
PY - 1986/5/1
Y1 - 1986/5/1
N2 - A series of 5′-halogenated formycins, including the chloro-, bromo- and iodo- derivatives, were synthesized. These compounds are competitive inhibitors of 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAPase) with Ki values in the range of 10−7 M, making them the most potent inhibitors of MTAPase reported to date. These compounds protect cells from the growth-inhibitory action of 5′-halogenated adenosines, which must be activated by MTAPase. The syntheses of 5′-halogenated formycin B derivatives, which inhibit purine nucleoside phosphorylase, are also described.
AB - A series of 5′-halogenated formycins, including the chloro-, bromo- and iodo- derivatives, were synthesized. These compounds are competitive inhibitors of 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAPase) with Ki values in the range of 10−7 M, making them the most potent inhibitors of MTAPase reported to date. These compounds protect cells from the growth-inhibitory action of 5′-halogenated adenosines, which must be activated by MTAPase. The syntheses of 5′-halogenated formycin B derivatives, which inhibit purine nucleoside phosphorylase, are also described.
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U2 - 10.1080/07328318608068672
DO - 10.1080/07328318608068672
M3 - Article
AN - SCOPUS:0022608020
SN - 0732-8311
VL - 5
SP - 185
EP - 200
JO - Nucleosides and Nucleotides
JF - Nucleosides and Nucleotides
IS - 2
ER -