title: Synthesis and antitumor activities of derivatives of the marine mangrove fungal metabolite deoxybostrycin.
abstract: Deoxybostrycin (1) is an anthraquinone compound derived from the marine mangrove fungus Nigrospora sp. No. 1403 and has potential to be a lead for new drugs because of its various biological properties. A series of new derivatives (2-22) of deoxybostrycin were synthesized. The in vitro cytotoxicity of all the new compounds was tested against MDA-MB-435, HepG2 and HCT-116 cancer cell lines. Most of the compounds exhibit strong cytotoxicity with IC₅₀ values ranging from 0.62 to 10 μM. Compounds 19, 21 display comparable cytotoxicity against MDA-MB-435 to epirubicin, the positive control. The primary screening results indicate that the deoxybostrycin derivatives might be a valuable source of new potent anticancer drug candidates.
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-sen University, 135 Xingang West Road, Guangzhou 510275, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Chen
authors.forename: Xun
authors.initials: X
authors.lastname: Zhu
authors.forename: Li-Li
authors.initials: LL
authors.lastname: Zhong
authors.forename: Bing
authors.initials: B
authors.lastname: Yang
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.forename: Jue-Heng
authors.initials: JH
authors.lastname: Wu
authors.forename: Sheng-Ping
authors.initials: SP
authors.lastname: Chen
authors.forename: Yong-Cheng
authors.initials: YC
authors.lastname: Lin
authors.forename: Yuhua
authors.initials: Y
authors.lastname: Long
authors.forename: Zhi-Gang
authors.initials: ZG
authors.lastname: She
mesh_terms: D000880:Anthraquinones / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D001203:Ascomycota / Q000737:chemistry*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000473:pathology; D015251:Epirubicin / Q000494:pharmacology; D005260:Female; D045325:HCT116 Cells; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology
chemical_list: D000880:Anthraquinones; D000970:Antineoplastic Agents; C034288:4-deoxybostrycin; D015251:Epirubicin