Synthesis and activity of pyrimidinylpropenamide antibiotics: the alkyl analogues of sparsomycin.
Facile syntheses of sparsomycin (3) and its four analogues (4-7) based on diastereoselective oxidation of sulfide, sulfenylation, and coupling of 6-methyluracylacryllic acid with monooxodithioacetal amine, are described. Studies on the biological activity of morphological reversion on src(ts)-NRK cells were also carried out.
Nakajima
Noriyuki
N
Biotechnology Research Center, Toyama Prefectural University, Kosugi, Japan. nori@pu-toyama.ac.jp
Enomoto
Takeshi
T
Watanabe
Takehiro
T
Matsuura
Nobuyasu
N
Ubukata
Makoto
M
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000494:pharmacology*; D001358:Avian Sarcoma Viruses / Q000378:metabolism; D002471:Cell Transformation, Neoplastic / Q000187:drug effects*; D051379:Mice; D010084:Oxidation-Reduction; D013033:Sparsomycin / Q000138:chemical synthesis / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D013033:Sparsomycin