title: A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes.
abstract: We have screened 11 isoquinoline derivatives and α-methylene-γ-butyrolactones using the 3-(4,5-dimethylthi-azol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HeLa and HEK-293T cells. Compound 2 was identified as potential anticancer agent. To further improve its therapeutic potential, this agent was incorporated into transferrin (Tf)-conjugated liposomes (LPs) for targeted delivery to tumor cells. We have demonstrated Tf-LP-Compound 2 have superior antitumor activity compared to non-targeted controls and the free drug. These data show Tf-LP-Compound 2 to be a promising agent that warrants further evaluation.
authors: College of Life Sciences, Jilin University, Changchun, China.
authors: Xuewei
authors: X
authors: Yang
authors: College of Life Sciences, Jilin University, Changchun, China.
authors: Shuang
authors: S
authors: Yang
authors: College of Life Sciences, Jilin University, Changchun, China.
authors: Hongyu
authors: H
authors: Chai
authors: College of Pharmacy, The Ohio State University, Columbus, United States of America.
authors: Zhaogang
authors: Z
authors: Yang
authors: College of Life Sciences, Jilin University, Changchun, China; College of Pharmacy, The Ohio State University, Columbus, United States of America.
authors: Robert J
authors: RJ
authors: Lee
authors: Department of Organic Chemistry, College of Chemistry, Jilin University, Changchun, China.
authors: Weiwei
authors: W
authors: Liao
authors: College of Life Sciences, Jilin University, Changchun, China.
authors: Lesheng
authors: L
authors: Teng
mesh_terms: D000179:Acrylates / Q000008:administration & dosage* / Q000737:chemistry; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers; D004354:Drug Screening Assays, Antitumor; D004705:Endocytosis; D057809:HEK293 Cells; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D007546:Isoquinolines / Q000008:administration & dosage* / Q000737:chemistry; D007783:Lactones / Q000737:chemistry / Q000494:pharmacology; D008081:Liposomes; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D011804:Quinolines / Q000008:administration & dosage* / Q000737:chemistry; D011990:Receptors, Transferrin / Q000378:metabolism; D014168:Transferrin / Q000737:chemistry*
chemical_list: D000179:Acrylates; D000970:Antineoplastic Agents; D004337:Drug Carriers; D007546:Isoquinolines; D007783:Lactones; D008081:Liposomes; D011804:Quinolines; D011990:Receptors, Transferrin; D014168:Transferrin