title: Synthesis and cytotoxicity of (-)-renieramycin G analogs.
abstract: (-)-Renieramycin G and fifteen C-22 analogs were prepared employing l-tyrosine as the chiral starting material. These analogs, along with (-)-renieramycin G itself, were evaluated in vitro for cytotoxicity against HCT-8, BEL-7402, A2780, MCF-7, A549, BGC-823, Ketr3, KB, Hela cells. The IC(50) values of most of these analogs were at the level of μM. Among these analogs, 2-thiophenecarboxylate ester derivative 17 exhibited potent cytotoxic activity against KB cell line with the IC(50) of 20 nM. From this study, it could be concluded that the C-22 side chain played an important role in the cytotoxic potency and specificity of this class of (-)-renieramycin G derivatives.
authors.affiliation: Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine (Ministry of Education), Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing, People's Republic of China.
authors.forename: Wei
authors.initials: W
authors.lastname: Liu
authors.forename: Wenfang
authors.initials: W
authors.lastname: Dong
authors.forename: Xiangwei
authors.initials: X
authors.lastname: Liao
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yan
authors.forename: Baohe
authors.initials: B
authors.lastname: Guan
authors.forename: Nan
authors.initials: N
authors.lastname: Wang
authors.forename: Zhanzhu
authors.initials: Z
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D044005:Tetrahydroisoquinolines; C507294:renieramycin G