title: Parallel solution-phase synthesis of an adenosine antibiotic analog library.
abstract: A library of eighty one adenosine antibiotic analogs was prepared under the Pilot Scale Library Program of the NIH Roadmap initiative from 5'-amino-5'-deoxy-2',3'-O-isopropylidene-adenosine 3. Diverse aldehyde, sulfonyl chloride and carboxylic acid reactant sets were condensed to 3, in solution-phase fashion, leading after acid-mediated hydrolysis to the targeted compounds in good yields and high purity. No marked antituberculosis or anticancer activity was noted on preliminary cellular testing, but these nucleoside analogs should be useful candidates for other types of biological activity.
authors: Southern Research Institute, Drug Discovery Division, Birmingham, AL 35205, USA. moukhachafiq@southernresearch.org
authors: Omar
authors: O
authors: Moukha-chafiq
authors: Robert C
authors: RC
authors: Reynolds
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D019073:HT29 Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D012996:Solutions; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D000995:Antitubercular Agents; D012996:Solutions; D000241:Adenosine
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