title: Synthesis of isatin thiosemicarbazones derivatives: in vitro anti-cancer, DNA binding and cleavage activities.
abstract: New derivatives of thiosemicarbazone Schiff base with isatin moiety were synthesized L1-L6. The structures of these compounds were characterized based on the spectroscopic techniques. Compound L6 was further characterized by XRD single crystal. The interaction of these compounds with calf thymus (CT-DNA) exhibited high intrinsic binding constant (k(b)=5.03-33.00×10(5) M(-1)) for L1-L3 and L5 and (6.14-9.47×10(4) M(-1)) for L4 and L6 which reflect intercalative activity of these compounds toward CT-DNA. This result was also confirmed by the viscosity data. The electrophoresis studies reveal the higher cleavage activity of L1-L3 than L4-L6. The in vitro anti-proliferative activity of these compounds against human colon cancer cell line (HCT 116) revealed that the synthesized compounds (L3, L6 and L2) exhibited good anticancer potency.
authors.affiliation: School of Chemical Sciences, Universiti Sains Malaysia, Minden 11800, Pulau Pinang, Malaysia.
authors.forename: Amna Qasem
authors.initials: AQ
authors.lastname: Ali
authors.affiliation: School of Chemical Sciences, Universiti Sains Malaysia, Minden 11800, Pulau Pinang, Malaysia. Electronic address: sgteoh@usm.my.
authors.forename: Siang Guan
authors.initials: SG
authors.lastname: Teoh
authors.affiliation: School of Chemical Sciences, Universiti Sains Malaysia, Minden 11800, Pulau Pinang, Malaysia.
authors.forename: Abdussalam
authors.initials: A
authors.lastname: Salhin
authors.affiliation: Department of Chemistry, Sciences & Arts College - Rabigh, King AbdullAziz University, Rabigh, Saudi Arabia.
authors.forename: Naser Eltaher
authors.initials: NE
authors.lastname: Eltayeb
authors.affiliation: EMAN Research and Testing Laboratory, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Pulau Pinang, Malaysia.
authors.forename: Mohamed B
authors.initials: MB
authors.lastname: Khadeer Ahamed
authors.affiliation: EMAN Research and Testing Laboratory, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Pulau Pinang, Malaysia.
authors.forename: A M S
authors.initials: AM
authors.lastname: Abdul Majid
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D053837:DNA Cleavage / Q000187:drug effects*; D004273:DNA, Neoplasm / Q000378:metabolism*; D045325:HCT116 Cells; D006801:Humans; D006868:Hydrolysis / Q000187:drug effects; D007510:Isatin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D008968:Molecular Conformation; D010084:Oxidation-Reduction / Q000187:drug effects; D010957:Plasmids / Q000378:metabolism; D013050:Spectrometry, Fluorescence; D013055:Spectrophotometry, Infrared; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014783:Viscosity / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D013882:Thiosemicarbazones; D007510:Isatin
keywords: CT-DNA binding; DNA cleavage; In vitro anti-proliferative activity; Isatin moiety; Thiosemicarbazone