title: Synthesis and cytotoxicity study of novel 3-(triazolyl)coumarins based fluorescent scaffolds.
abstract: Recently a choice of fluorescent bioimaging probes have been developed as medical diagnostic tools. Herein, we have introduced a series of coumarin-based target specific probes for cancer theranostic application which play a dual role in the field of both diagnosis and therapy. A fluorogenic version of 1,3-dipolar cycloaddition between azides and alkynes (DBCO) has been introduced to develop the triazolylcoumarin based fluorescent scaffolds. These scaffolds were screened for their anticancer activity against breast cancer (MCF7) and human epitheloid cervix carcinoma (HeLa) cell line. It was established that triazolylcoumarins (5c and 5d) are having electronegative substitution in the benzene ring displayed most effective anticancer profile in both the cell lines. Compounds 5a and 5d exhibited maximum quantum yield and strong cellular uptake in the MCF-7 cell line.
authors: Department of Chemistry, School of Advanced Sciences, VIT University, Vellore 632014, India.
authors: Sohini
authors: S
authors: Sinha
authors: Department of Chemistry, School of Advanced Sciences, VIT University, Vellore 632014, India.
authors: Anuja Plavuvalapil
authors: AP
authors: Kumaran
authors: School of Bioscience & Technology, VIT University, Vellore 632014, Tamil Nadu, India.
authors: Debasish
authors: D
authors: Mishra
authors: Department of Chemistry, School of Advanced Sciences, VIT University, Vellore 632014, India. Electronic address: priyankar.paira@vit.ac.in.
authors: Priyankar
authors: P
authors: Paira
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000175:diagnosis / Q000188:drug therapy; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology*; D061565:Cycloaddition Reaction; D005260:Female; D005456:Fluorescent Dyes / Q000737:chemistry / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D061848:Optical Imaging / Q000379:methods; D000068936:Theranostic Nanomedicine; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*; D002583:Uterine Cervical Neoplasms / Q000175:diagnosis / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins; D005456:Fluorescent Dyes; D014230:Triazoles
keywords: Anticancer activity; Fluorescence imaging; Fluorescence study; Theranostic application; Triazolylcoumarin