title: Cytotoxic activities of new jadomycin derivatives.
abstract: Cytotoxic activities of jadomycin B and five new jadomycin derivatives against four cancer cell lines (HepG2, IM-9, IM-9/Bcl-2 and H460) were evaluated. Jadomycin S was most potent against HepG2, IM-9 and IM-9/Bcl-2 while jadomycin F was most potent against H460. Their potencies correlated with the degrees of apoptosis induced. Structure-activity-relationship analyses clearly demonstrate that the side chains of the oxazolone ring derived from the incorporated amino acids make a significant impact on biological activity. Therefore, jadomycin offers an ideal scaffold to manipulate structure and could be exploited to make many novel bioactive compounds with altered activities.
authors.affiliation: State Key Laboratory of Microbial Resources, Institute of Microbiology, Chinese Academy of Sciences, Beijing, 100080, PR. China.
authors.forename: Jian-Ting
authors.initials: JT
authors.lastname: Zheng
authors.forename: Uwe
authors.initials: U
authors.lastname: Rix
authors.forename: Lixia
authors.initials: L
authors.lastname: Zhao
authors.forename: Cynthia
authors.initials: C
authors.lastname: Mattingly
authors.forename: Val
authors.initials: V
authors.lastname: Adams
authors.forename: Quan
authors.initials: Q
authors.lastname: Chen
authors.forename: Jürgen
authors.initials: J
authors.lastname: Rohr
authors.forename: Ke-Qian
authors.initials: KQ
authors.lastname: Yang
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry / Q000633:toxicity*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007546:Isoquinolines / Q000737:chemistry / Q000633:toxicity; D013302:Streptomyces / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000903:Antibiotics, Antineoplastic; D007546:Isoquinolines; C081750:jadomycin B