Facile synthesis of some novel pyrido[3',2':4,5]thieno[2,3-b][1,4]thiazine-8-carboxylic acids

Molecules. 2007 Mar 15;12(3):497-503. doi: 10.3390/12030497.

Abstract

Model tetrahydropyrido[3',2':4,5]thieno[2,3-b][1,4]thiazines 9a-c were synthesized via reductive lactamization, using sodium dithionite, of the respective 2-[(carboxyalkyl)thio]-3-nitro-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acids 7a-c. The latter derivatives were made via interaction of 2-chloro-7-cyclopropyl-3-nitro-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid (6) with each of alpha-mercaptoacetic, alpha-mercaptopropionic, and alpha-mercaptosuccinic acids and triethylamine in aqueous acetone at room temperature. The structures of 7a-7c and 9a-9c are supported by microanalytical and spectral (IR, MS, NMR) data. Compounds 9a and 9c showed potent inhibitory activity against the IGROV1 (Ovarian Cancer) cell line.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Carboxylic Acids / chemical synthesis*
  • Carboxylic Acids / chemistry
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Thiazines / chemical synthesis*
  • Thiazines / chemistry
  • Thiophenes / chemical synthesis*
  • Thiophenes / chemistry

Substances

  • Antineoplastic Agents
  • Carboxylic Acids
  • Thiazines
  • Thiophenes