title: Design and synthesis of novel thiophenes bearing biologically active aniline, aminopyridine, benzylamine, nicotinamide, pyrimidine and triazolopyrimidine moieties searching for cytotoxic agents.
abstract: To discover new bioactive lead compounds for medicinal purposes, herein, (E)-3-(substituted amino)-1-thiophen-2-yl-prop-2-en-1-ones 3-8, aminopyridines 9-11, benzylamine 12, nicotinamide 13, pyrimidines 14, 15, hexanoic acid 16 and triazolopyrimidine 19 were prepared and tested for cytotoxic activity. Results showed that the tested compounds exhibited a remarkable activity, especially compounds 3 and 19 with IC50 values (55.2 and 50.49 microM, respectively) compared to doxorubicin (IC50 = 71.8 microM) as a reference drug.
authors.forename: Mostafa M
authors.initials: MM
authors.lastname: Ghorab
authors.forename: Marwa G
authors.initials: MG
authors.lastname: El-Gazzar
authors.forename: Mansour S
authors.initials: MS
authors.lastname: Alsaid
mesh_terms: D000631:Aminopyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001596:Benzylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D015394:Molecular Structure; D009536:Niacinamide / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000631:Aminopyridines; D000814:Aniline Compounds; D000970:Antineoplastic Agents; D001596:Benzylamines; D011743:Pyrimidines; D013876:Thiophenes; D014230:Triazoles; D009536:Niacinamide