2. Academic Validation
  3. Indolylmethylene benzo[h]thiazolo[2,3-b]quinazolinones: synthesis, characterization and evaluation of anticancer and antimicrobial activities

Indolylmethylene benzo[h]thiazolo[2,3-b]quinazolinones: synthesis, characterization and evaluation of anticancer and antimicrobial activities

  • Bioorg Med Chem Lett. 2014 Sep 1;24(17):4239-42. doi: 10.1016/j.bmcl.2014.07.030.
Rajitha Gali 1,  Janardhan Banothu 1,  Mahendar Porika 2,  Ravibabu Velpula 1,  Sairengpuii Hnamte 3,  Rajitha Bavantula 4,  Sadanandam Abbagani 2,  Siddhardha Busi 3
Affiliations

Affiliations

  • 1 Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India.
  • 2 Department of Bio-Technology, Kakatiya University, Warangal 506009, Telangana, India.
  • 3 Centre for Microbiology, School of Life Sciences, Pondicherry University, Puducherry 605014, India.
  • 4 Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India. Electronic address: rajitabhargavi@yahoo.com.
PMID: 25096298 DOI: 10.1016/j.bmcl.2014.07.030
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.

Keywords

Anticancer activity; Antimicrobial activity; Indole-3-carbaldehyde; Thiazolo[2,3-b]quinazolinone.

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