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Abstract

Reaction of 1H-indole-3-carboxaldhyde (1) with thiosemicarbazide derivatives to give thiosemicarbazone derivatives (2a,b). Cyclization of thiosemicarbazone (2a) with HCl, Ac2O, phenacyl bromides and chloroacetic acid afforded the corresponding 1,2,4-triazole-3-thiol (3), diacetyl derivative (4), 1.3-thiazole derivative (5) and 1,3-thiazolidin- 4-ones derivative (6), respectively. Compound 6 undergoes a series of heterocyclization reactions to give new heterocyclic compounds. The structures of newly synthesized compounds had been confirmed by elemental analysis and spectral data. Some of newly synthesized compounds were evaluated for in vitro cytotoxic activity against three human cancer cell lines, including human liver cancer (Hep G2), humam colon cancer (HT-29) and human breast cancer (MCF-7) using MTT assay.

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Thiosemicarbazone Cytotoxic activity MTT assay 1.3-Thiazole 1,3-Thiazoldinone Pyrazolo[3,4-d]1,3-thiazole

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S. Salman, A., A. Mahmoud, N., A. Mohamed, M., Abdel-Aziem, A., & M. Elsisi, D. (2017). Synthesis, Characterization and in vitro Cytotoxic Evaluation of Some Novel Heterocyclic Compounds Bearing Indole Ring. Asian Journal of Organic & Medicinal Chemistry, 2(1), 42–52. https://doi.org/10.14233/ajomc.2017.AJOMC-P66
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