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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
chemistry
New approaches for the synthesis of pyrazole, thiophene, thieno[2,3-b]pyridine, and thiazole derivatives together with their anti-tumor evaluations
Medicinal Chemistry Research, Volume 23, No. 2, Year 2014
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Description
The reaction of cyanoacetylhydrazine (1) with acetylchloride (2) gave the N-acyl derivative 3. The latter underwent ready cyclization in sodium ethoxide to give the pyrazole derivative 4 which was the key compound for the synthesis of thiophene, thieno[2,3-b]pyridine, and thiazole derivatives. The anti-tumor evaluations of the newly synthesized products against the three human tumor cell lines, namely, breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460), and CNS cancer (SF-268), were studied. Some of these compounds were found to exhibit much higher inhibitory effects toward the three tumor cell lines than the reference doxorubicin. Molecular modeling of the four compounds 12c, 12f, 16a, and 16d, which showed the maximum inhibitory effect, were done. © 2013 Springer Science+Business Media New York.
Authors & Co-Authors
Mohareb, Rafat Milad
Egypt, Giza
Faculty of Science
Abdallah, Amira Elsayed Mahmoud
Egypt, Helwan
Faculty of Science
Abdelaziz, Mahmoud A.
Saudi Arabia, Riyadh
Al-ghad International Colleges for Applied Medical Sciences
Egypt, Cairo
Modern Academy for Engineering and Technology in Maadi
Statistics
Citations: 48
Authors: 3
Affiliations: 4
Identifiers
Doi:
10.1007/s00044-013-0664-7
ISSN:
10542523
Research Areas
Cancer