Synthesis and evaluation of some novel benzothiazole derivatives as potential anticancer and antimicrobial agents

Arzneimittelforschung. 2007;57(8):547-53. doi: 10.1055/s-0031-1296647.

Abstract

Intensive efforts are underway worldwide to develop anticancer and antimicrobial agents. Therefore, a novel series of pyrido[2,1-b]benzo [d]thiazole and 2-(benzo [d] thiazol-2-ylamino)pyrimidine derivatives was synthesized. The synthesized compounds were evaluated for their anticancer activity. Among the tested compounds, compounds 3a, 3b, and 7 exhibited more cytotoxic action than the control drug doxorubicin (CAS 23214-92-8; IC50: 52 microg/ml). Compound 7 was the most potent cytotoxic, with an IC50 of 42.55 pg/ ml, while compounds 3a and 3b induced high cytotoxic action with IC50 values of 50.15 pg/ml and 50.45 pg/ml, respectively. Moreover, the synthesized compounds were screened for their antibacterial and antifungal activities. Compound 6 exhibited moderate antifungal activity against C. albicans with a minimum inhibitory concentration of 125 pg/ml.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / pharmacology*
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Bacteria / drug effects
  • Benzothiazoles / chemical synthesis*
  • Benzothiazoles / pharmacology*
  • Carcinoma, Ehrlich Tumor / drug therapy
  • Cell Count
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Chemical Phenomena
  • Chemistry, Physical
  • Drug Screening Assays, Antitumor
  • Female
  • Fungi / drug effects
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Mice
  • Microbial Sensitivity Tests
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Antifungal Agents
  • Antineoplastic Agents
  • Benzothiazoles
  • Indicators and Reagents