Synthesis and evaluation of biological activities of a series of (6-substituted benzothiazol-2-yl)acrylamides

Med Chem. 2011 Nov;7(6):727-31. doi: 10.2174/157340611797928280.

Abstract

A series of simple (6-substituted benzothiazol-2-yl)acrylamides was synthesized and evaluated for cytotoxicity and antimicrobial effects. All six compounds displayed very significant cytotoxicity against four cancer cell lines tested including A549 (a human lung cancer cell line), Hela (a human ovarian cancer cell line), MCF7 (a human breast cancer cell line), and even MCF7-ADR (adriamycin-resistant human breast cancer cell line), with IC(50) values in microgram/ml range and as low as 0.66 μg/ml. The synthesized compounds also exhibited some antifungal effects against Apergillus niger.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylamides / chemical synthesis
  • Acrylamides / chemistry
  • Acrylamides / pharmacology*
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Bacteria / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Fungi / drug effects*
  • HeLa Cells
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Acrylamides
  • Anti-Bacterial Agents
  • Antifungal Agents
  • Antineoplastic Agents