title: Synthesis of retinoid enhancers based on 2-aminobenzothiazoles for anti-cancer therapy.
abstract: Indole-3-amides and dipeptides were produced from 2-aminobenzothiazoles using the PyBop peptide coupling reagent. These analogues were tested in anti-cancer cell viability assays against SH-SY5Y neuroblastoma and MDA-MB-231 breast adenocarcinoma cell lines, and were found to exhibit cytotoxic activities at concentrations ranging from 0.1 to 20μM. These compounds were also found to act additively with a low dosage of 13-cis-retinoic acid in neuroblastoma cells. Then, using neuroblastoma cells transfected to stably overexpress the RARβ(2) gene, a SAR was developed for the indole-3-amides. Real-time PCR was also used to demonstrate their RARβ(2) agonistic activity.
authors.affiliation: School of Chemistry, The University of New South Wales, Sydney, NSW, Australia.
authors.forename: Christopher R
authors.initials: CR
authors.lastname: Gardner
authors.forename: Belamy B
authors.initials: BB
authors.lastname: Cheung
authors.forename: Jessica
authors.initials: J
authors.lastname: Koach
authors.forename: David StC
authors.initials: DS
authors.lastname: Black
authors.forename: Glenn M
authors.initials: GM
authors.lastname: Marshall
authors.forename: Naresh
authors.initials: N
authors.lastname: Kumar
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D002470:Cell Survival; D004151:Dipeptides / Q000138:chemical synthesis / Q000737:chemistry; D005260:Female; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015474:Isotretinoin / Q000494:pharmacology*; D009447:Neuroblastoma / Q000188:drug therapy; D018168:Receptors, Retinoic Acid / Q000819:agonists*
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles; D004151:Dipeptides; D007211:Indoles; D018168:Receptors, Retinoic Acid; C523775:aminobenzothiazole compound; C540966:retinoic acid receptor, beta2, human; D015474:Isotretinoin