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Anticancer activity of novel Schiff bases and azo dyes derived from 3-amino-4-hydroxy-2H-pyrano[3,2-c]quinoline-2,5(6H)-dione

Abdeltawab M. Saeed, Shaikha S. AlNeyadi, Ibrahim M. Abdou

2020Heterocyclic Communications43 citationsDOIOpen Access PDF

Abstract

Abstract New Schiff bases and azo dyes derivatives have been synthesized via appropriate conventional methods using pyranoquinolinone as a starting material. The compounds obtained were characterized by spectral analysis and evaluated for anticancer activity in several human tumor cell lines: MCF-7 breast cancer, HepG2 liver cancer and HCT-116 colon carcinoma. 5-fluorouracil was used as a reference drug. The in vitro cytotoxicity screening results revealed that all tested compounds showed promising activity against MCF-7 cells. In particular, compounds 6a, 6b , and 7b showed excellent activity against the three human tumor cell lines. Structure-activity relationship studies indicated that the azo derivative with a trifluoromethoxy group (compound 7b ) was the most potent candidate against the three human tumor cell lines (IC 50 , 1.82-8.06 μg/mL). Our findings highlight pyranoquinolinone analogues as a promising class of compounds for new anticancer therapies.

Topics & Concepts

ChemistryQuinolineCytotoxicityIn vitroCombinatorial chemistryStereochemistryCell cultureDerivative (finance)Schiff baseCancer cell linesHuman breastCancer cellCancerBiochemistryOrganic chemistryMedicineGeneticsInternal medicineFinancial economicsBiologyEconomicsSynthesis and biological activitySynthesis and Biological EvaluationBioactive Compounds and Antitumor Agents
Anticancer activity of novel Schiff bases and azo dyes derived from 3-amino-4-hydroxy-2H-pyrano[3,2-c]quinoline-2,5(6H)-dione | Litcius