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. 2021 Feb 22;3(8):2157–2179. doi: 10.1039/d0na01084g

A list of chemotherapeutic nucleosidic analogs in clinical trials.

Name Structure Statusa Chemical modification Targeted cancer Mechanism of action
Tezacitabine graphic file with name d0na01084g-u10.jpg Phase I/II trials • Sugar ring modification by fluoro-methylene-halogenation • Refractory solid tumors • Enzymatic inhibition 43
Troxacitabine graphic file with name d0na01084g-u11.jpg Phase I/II trials • Sugar ring modification by dihydroxylation • Acute myelogenous leukemia (AML) • Inhibitor of DNA polymerases 44 and 45
l-Enantiomer
rx-3117 graphic file with name d0na01084g-u12.jpg Phase I/II trials • Sugar replacement by a cyclopentene ring and F-halogenation • Metastatic bladder cancer • DNA hypomethylation 46 and 47
• Metastatic pancreatic cancer
8-Chloroadenosine graphic file with name d0na01084g-u13.jpg Phase I/II trials • Adenine modification by Cl-halogenation • Recurrent acute myeloid leukemia • Enzymatic inhibition 48
a

Trial status was verified by the NIH – U.S. National Library of Medicine clinical trials database (http://www.clinicaltrials.gov).