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5. Pure monophasic, epithelial synovial sarcoma without a spindle cell component

Author

Katsushi Tajima, Fuyama S, Akiba J, Katoh T, Shinji Satoh, Akito Yahagi, Ohrui H, Suzuki K, Tomohiro Hayashi, and Yamaguchi H

Subjects
Pathology, medicine.medical_specialty, Histology, medicine.anatomical_structure, business.industry, Component (thermodynamics), Cell, medicine, General Medicine, Epithelial Synovial Sarcoma, business, Pathology and Forensic Medicine
Published
1999
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25. Syntheses of 4‘-C-Ethynyl-β-<SCP>d</SCP>-arabino- and 4‘-C-Ethynyl-2‘-deoxy-β-<SCP>d</SCP>-ribo-pentofuranosylpyrimidines and -purines and Evaluation of Their Anti-HIV Activity

Author

Ohrui, H., Kohgo, S., Kitano, K., Sakata, S., Kodama, E., Yoshimura, K., Matsuoka, M., Shigeta, S., and Mitsuya, H.

Abstract

4‘-C-Ethynyl-β-d-arabino- and 4‘-C-ethynyl-2‘-deoxy-β-d-ribo-pentofuranosylpyrimidine and -purine nucleosides were synthesized and evaluated for their in vitro anti-HIV activity. The key intermediate, 4-C-ethynyl- or 4-C-triethylsilylethynyl-d-ribo-pentofuranose, was prepared from d-glucose and glycosidated with various pyrimidine or purine bases. The arabino pyrimidine derivatives were prepared from the corresponding ribo derivatives via O2,2‘-anhydro nucleosides. The 2‘-deoxy-ribo derivatives were synthesized by radical reduction of 2‘-bromo or 2‘- phenoxythiocarbonyloxy nucleosides. Among these 4‘-C-ethynyl nucleosides, seven analogues proved to be potent against HIV-1 in vitro with EC50 values ranging from 0.0003 to 0.03 μM. These compounds also exerted activity against clinical and multi-dideoxy-nucleoside-resistant HIV-1 strains with comparable EC50 values. Three such 4‘-C-ethynyl-2‘-deoxypurine analogues including 4‘-C-ethynyl-2‘-deoxyadenosine and 4‘-C-ethynyl-2,6-diamino-2‘-deoxypurine were less cytotoxic [selectivity indices (SIs):  975−2733] than three 4‘-C-ethynyl-2‘-deoxycytidine analogues (SIs:  63−363). 4‘-C-Ethynyl-5-fluoro-2‘-deoxycytidine was least toxic (SI:  >3333) and potent against all HIV strains tested.

Published
2000

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