title: One-pot multicomponent synthesis of indole incorporated thiazolylcoumarins and their antibacterial, anticancer and DNA cleavage studies.
abstract: A series of indole incorporated thiazolylcoumarins (7a-q) have been synthesized and evaluated for their antibacterial, anticancer and DNA cleavage studies. Analysis of antibacterial studies indicated that all the synthesized compounds possess promising activity towards the screened bacterial strains. In vitro anticancerous action was studied for compound 7a (NSC: 768621/1) against the full panel of 60 human tumor cell lines. The five dose level activity results revealed that, the compound 7a was active against all the cell lines among them it has shown potent activity against Leukemia: CCRF-CEM (GI₅₀: 0.33 μM), Non-Small Cell Lung Cancer: NCI-H522 (GI₅₀: 1.03 μM), Colon Cancer: HCT-116 (GI₅₀: 1.60 μM), CNS Cancer: SF-539 (GI₅₀: 1.58 μM), Melanoma MALME-3M (GI50: 1.59 μM), Ovarian Cancer: OVCAR-3 (GI₅₀: 1.16 μM), Renal Cancer: UO-31 (GI₅₀: 0.76 μM), Prostate Cancer: PC-3 (GI₅₀: 0.82 μM) and Breast Cancer: BT-549 (GI₅₀: 1.13 μM). DNA cleavage studies revealed that even at 50 μg/mL concentration complete DNA digestion was observed for all the compounds, except for compound (7o) where partial DNA digestion was observed even at 100 μg/mL.
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India.
authors.forename: Rajitha
authors.initials: R
authors.lastname: Gali
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India.
authors.forename: Janardhan
authors.initials: J
authors.lastname: Banothu
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India.
authors.forename: Ramesh
authors.initials: R
authors.lastname: Gondru
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India. Electronic address: rajitabhargavi@yahoo.com.
authors.forename: Rajitha
authors.initials: R
authors.lastname: Bavantula
authors.affiliation: Department of Bio-Technology, Kakatiya University, Warangal 506009, Telangana, India.
authors.forename: Yashodhara
authors.initials: Y
authors.lastname: Velivela
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA.
authors.forename: Peter A
authors.initials: PA
authors.lastname: Crooks
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects / Q000502:physiology; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology; D053837:DNA Cleavage / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D003374:Coumarins; D007211:Indoles; D013844:Thiazoles; C030374:indole
keywords: Antibacterial activity; Anticancer activity; DNA cleavage studies; Indoles; Thiazolylcoumarins