Synthesis and Antitumor Activity of Some New Fused Heterocyclic Compounds
- 作者: El-Hag F.1, Abdel-Hafez N.2, Abbas E.1, El-Manawaty M.3, El-Rashedy A.1
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隶属关系:
- Department of Chemistry of Natural and Microbial Products
- Applied Organic Chemistry Department
- Pharmacognosy Department
- 期: 卷 89, 编号 1 (2019)
- 页面: 128-137
- 栏目: Article
- URL: https://journals.rcsi.science/1070-3632/article/view/222720
- DOI: https://doi.org/10.1134/S1070363219010237
- ID: 222720
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详细
Reaction of thiopyrimidine derivative 3 with hydrozonoyl chlorides 4a–4e gives new fused heterocyclic compounds 7a–7e containing triazole ring. The latter demonstrates a wide range of biological activities. Thiazolone pyridopyrimidines 8, 9a, 9b are prepared by the reaction of thiopyrimidines with chloroacetic acid and different aromatic aldehydes in the presence of acetic anhydride. Bis-arylidene 2 reacts with malononitrile or ethyl cyanoacetate with formation of carbonitrile derivatives 10, 11. Reaction of bisarylidene 2 with phenyl hydrazine and hydrazine hydrate leads to diazole derivatives 12, 13. Structures of the new compounds are elucidated from IR, 1H and 13C NMR, and mass spectra. All newly synthesized products are tested for antitumor activity on three human tumor cell lines, including prostatic adenocarcinoma (PC3), human colorectal carcinoma (HCT116), human liver hepatocellular carcinoma (HepG2) and breast carcinoma (MCF7). Compounds 2, 7a–7d demonstrate the considerable potency.
作者简介
F. El-Hag
Department of Chemistry of Natural and Microbial Products
编辑信件的主要联系方式.
Email: fatmaabdaleem@yahoo.com
埃及, Dokki, Cairo, 12622
N. Abdel-Hafez
Applied Organic Chemistry Department
Email: fatmaabdaleem@yahoo.com
埃及, Dokki, Cairo, 12622
E. Abbas
Department of Chemistry of Natural and Microbial Products
Email: fatmaabdaleem@yahoo.com
埃及, Dokki, Cairo, 12622
M. El-Manawaty
Pharmacognosy Department
Email: fatmaabdaleem@yahoo.com
埃及, Dokki, Cairo, 12622
A. El-Rashedy
Department of Chemistry of Natural and Microbial Products
Email: fatmaabdaleem@yahoo.com
埃及, Dokki, Cairo, 12622