Cytotoxic activities and morphological studies of thiophene, thiazole and pyridazine derivatives synthesized from benzo[d]thiazole derivatives

Authors

  • Karam Ahmed El-Sharkawy Pharmaceutical Chemistry Department, Pharmacy College, Jazan University, P.O. Box 114, Jazan, Saudi Arabia
  • Rafat Mohareb Chemistry Department, faculty of science, Cairo university http://orcid.org/0000-0003-3922-803X
  • Sayeed Muchtar Abdulhakim Department of Chemistry, Faculty of Science, University of Tabuk, Tabuk – 71491, Kingdom of Saudi Arabia
  • Humaira Parveen Nabi Department of Chemistry, Faculty of Science, University of Tabuk, Tabuk – 71491, Kingdom of Saudi Arabia
  • Mahmoud Ali Abdelaziz Department of Chemistry, Faculty of Science, University of Tabuk, Tabuk – 71491, Kingdom of Saudi Arabia

DOI:

https://doi.org/10.17344/acsi.2023.8057

Keywords:

Benzo[d]thiazole, thiophene, thiazole, pyridazine, cytotoxicity, morphological studies

Abstract

Abstract

       The benzo[d]thiazole derivatives 4a-c were synthesized and used for the synthesis of thiophene derivatives 6a-f. They form the arylhydrazone derivatives 8a-i which were capable to form pyridazine derivatives 9a-i and 10a-i. The latter compounds reacted with thioglycollic acid to produce the thiazole derivatives 12a-i and 13a-i, respectively. The thiazole derivatives 15a-c were also produced from 4a-c through their reactions with elemental sulfur and phenylisothiocyanate. Further heterocyclization reactions of 15a were carried out to produce thiophene derivatives.  Evaluations of the synthesized  products were carried out against some selected cancer cell lines and the most active compounds were further evaluated against the seventeen cancer cell lines classified according to the disease. Morphological changes of A549 cell line by the effect of compounds 13c and 13h were studied using microenvironment of the lung tissue where an excellent result was obtained.

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Published

26.08.2023

Issue

Section

Organic chemistry