title: Indolylmethylene benzo[h]thiazolo[2,3-b]quinazolinones: synthesis, characterization and evaluation of anticancer and antimicrobial activities.
abstract: A series of novel 10-((1H-indol-3-yl)methylene)-7-aryl-7,10-dihydro-5H-benzo[h]thiazolo[2,3-b]quinazolin-9(6H)-ones (8a-t) have been synthesized in good yields by the reaction of benzo[h]quinazoline-2(1H)-thiones (4a-f) with 2-chloro-N-phenylacetamide (5) followed by Knoevenagel condensation with various indole-3-carbaldehydes (7a-d) under conventional method. All the synthesized compounds were characterized by spectral studies and screened for their in vitro anticancer and antimicrobial activities. Compound 8c has exhibited excellent activity against MCF-7 (breast cancer cell line) than the standard drug Doxorubicin. Compound 8d against both the cancer cell lines, 8q against MCF-7 and 8c, 8h against HepG2 have also shown good activity. Remaining compounds have shown moderate activity against both the cell lines. Antimicrobial activity revealed that, the compound 8q and 8t against Staphylococcus aureus and 8i, 8k, 8l, 8q &8t against Klebsiella pneumoniae have shown equipotent activity on comparing with the standard drug Streptomycin. Remaining compounds have shown significant antibacterial and comparable antifungal activities against all the tested microorganisms.
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 Bio-Technology, Kakatiya University, Warangal 506009, Telangana, India.
authors.forename: Mahendar
authors.initials: M
authors.lastname: Porika
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India.
authors.forename: Ravibabu
authors.initials: R
authors.lastname: Velpula
authors.affiliation: Centre for Microbiology, School of Life Sciences, Pondicherry University, Puducherry 605014, India.
authors.forename: Sairengpuii
authors.initials: S
authors.lastname: Hnamte
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: Sadanandam
authors.initials: S
authors.lastname: Abbagani
authors.affiliation: Centre for Microbiology, School of Life Sciences, Pondicherry University, Puducherry 605014, India.
authors.forename: Siddhardha
authors.initials: S
authors.lastname: Busi
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001230:Aspergillus / Q000187:drug effects; D002175:Candida / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007711:Klebsiella pneumoniae / Q000187:drug effects; D061986:MCF-7 Cells; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D006576:Heterocyclic Compounds, 4 or More Rings; D011799:Quinazolines; D013844:Thiazoles
keywords: Anticancer activity; Antimicrobial activity; Indole-3-carbaldehyde; Thiazolo[2,3-b]quinazolinone