Mohareb R.M.El-Sayed N.N.E.Abdelaziz M.A.Departrment of ChemistryFaculty of ScienceCairo UniversityGiza 12613Egypt; Department of Organic ChemistryFaculty of PharmacyOctober University for Modern Sciences and Arts (MSA)El-Wahaat RoadOctober CityGiza 12411Egypt; National Organization for Drug Control and ResearchP.O. Box 29Cairo 11421Egypt; College of ScienceDepartment of ChemistryKing Saud UniversityRiyadh 11932Saudi Arabia; Preparatory Year DepartmentAL-Ghad International Colleges for Health SciencesTabuk MaleTabuk 41321Saudi Arabia; Basic Science DepartmentModern Academy for Engineering and Technology in MaadiMaadi 11431CairoEgypt2020-01-252020-01-25201214203049https://doi.org/10.3390/molecules17078449PubMedID22790561https://t.ly/P5WGMScopusThe reaction of cyanoacetylhydrazine with chloroacetyl chloride gave N?-(2-chloroacetyl)-2-cyanoacetohydrazide. The latter underwent cyclization to afford 1-(5 amino-3-hydroxy-1H-pyrazol-1-yl)-2-chloroethanone, which underwent nucleophilic substitution to give 3-(5-amino-3-hydroxy-1H- pyrazol-1-yl)-3-oxopropanenitrile. The latter two compounds were used as key synthons to synthesize new thiophene, pyran, thiazole and some fused heterocyclic derivatives. The antitumor activity of the newly synthesized compounds was evaluated against three human tumor cells lines, namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) and some of these compounds were found to exhibit much higher inhibitory effects towards the three tumor cell lines than the Gram positive control doxorubicin. � 2012 by the authors.EnglishAntitumorPyrazoleThiazoleThiopheneantineoplastic agentheterocyclic compoundhydrazine derivativepyrazolepyrazole derivativearticlechemistrydrug screeninghumanstructure activity relationsynthesistumor cell lineAntineoplastic AgentsCell Line, TumorDrug Screening Assays, AntitumorHeterocyclic CompoundsHumansHydrazinesPyrazolesStructure-Activity RelationshipArticlehttps://doi.org/10.3390/molecules17078449PubMedID22790561