title: Indole-2-carboxylic acid derived mono and bis 1,4-disubstituted 1,2,3-triazoles: Synthesis, characterization and evaluation of anticancer, antibacterial, and DNA-cleavage activities.
abstract: A series of new indole-2-carboxylic acid derived mono and bis 1,4-disubstituted 1,2,3 triazoles (I(1)-I(6) and I(7)-I(12)) were synthesized and screened for their anticancer (in vitro and in vivo), antibacterial, and DNA cleavage activities. All the synthesized compounds were characterized by spectral studies. The in vitro anticancer screening results revealed that compound I(12) has registered potential activity against MCF-7, HeLa and HEK293 as compared with the standard reference drug Cisplatin. Remaining compounds have exhibited moderate to good activity against three cancer cell lines. The antibacterial activity screening results revealed that compounds, I(6) and I(12) have registered excellent inhibition against Escherichia coli and Bacillus subtilis in comparison with the standard drug Streptomycin. Compounds I(2) and I(11) have partially cleaved the DNA at 100 μg mL(-1) concentration.
authors.affiliation: Department of Chemistry, Kakatiya University, Warangal, T.S. 506009, India.
authors.forename: Sirassu
authors.initials: S
authors.lastname: Narsimha
authors.affiliation: Department of Chemistry, Kakatiya University, Warangal, T.S. 506009, India.
authors.forename: Nukala
authors.initials: N
authors.lastname: Satheesh Kumar
authors.affiliation: Department of Chemistry, Kakatiya University, Warangal, T.S. 506009, India.
authors.forename: Battula
authors.initials: B
authors.lastname: Kumara Swamy
authors.affiliation: Department of Chemistry, Kakatiya University, Warangal, T.S. 506009, India. Electronic address: vasujac3@gmail.com.
authors.forename: Nagavelli
authors.initials: N
authors.lastname: Vasudeva Reddy
authors.affiliation: Department of Biotechnology, Kakatiya University, Warangal, T.S. 506009, India.
authors.forename: S K
authors.initials: SK
authors.lastname: Althaf Hussain
authors.affiliation: Chemical Biology Laboratory, Indian Institute of Chemical Technology, Hyderabad, T.S. 500007, India.
authors.forename: M
authors.initials: M
authors.lastname: Srinivasa Rao
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects; D002264:Carboxylic Acids; D049109:Cell Proliferation / Q000187:drug effects; D053837:DNA Cleavage / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004926:Escherichia coli / Q000187:drug effects; D057809:HEK293 Cells; D006367:HeLa Cells; D006801:Humans; D007211:Indoles / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D061986:MCF-7 Cells; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000473:pathology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D007211:Indoles; D014230:Triazoles; C058980:indole-2-carboxylic acid
keywords: 1,2,3-Triazoles; Antibacterial; Anticancer; DNA-cleavage activity; Indole 2-carboxylic acid