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Synthesis and in vitro Anti-tumor Activity of Some New Sebacoyl Chloride Based Heterocycles

[ Vol. 14 , Issue. 2 ]

Author(s):

Islam H. El Azab* and Nadia A.A. Elkanzi   Pages 309 - 320 ( 12 )

Abstract:


Background: N-Heterocycles are of special interest because, many natural and synthetic bioactive compounds are found to be N-containing heterocycles and they constitute an important class of pharmacophores in medicinal chemistry. Recently, 1,2,3-triazoles have been found to possess a vast range of vital applications in the agrochemical, pharmaceutical, and materials field. In addition, various compounds of the 1,2,3-triazole family have shown a broad spectrum of biological properties such as antibacterial, and anti-HIV activity. 1,3,4- Oxadiazoles are important oxygen and nitrogen containing heterocyclic compounds, they possess desirable electronic and charge-transport properties.

Methods: Two mammalian cell lines were grown in RPMI-1640 medium, supplemented with 10% heat inactivated FBS, 50 units/mL of penicillin and 50 g/mL of streptomycin and maintained at 37 °C in a humidified atmosphere containing 5% CO2. The cells were maintained as “monolayer culture” by serial sub-culturing. Preliminary cytotoxicity was performed using SRB method.

Results: Sebacoyl chloride and decanedihydrazide dihydrochloride are utilized as versatile building blocks to annulate a series of novel azole and/ or azine systems. The in vitro anti-tumor activities of the synthesized compounds were evaluated against human breast cancer cell line (MCF-7) and human cervical cancer cell line (HeLa). The obtained data indicated that the majority of the tested compounds possess significant anti-tumor activities against the tested tumor cell lines.

Conclusion: Sebacoyl chloride, decanedihydrazide dihydrochloride and N-nucleophiles are useful precursors for the synthesis of different functionalized N- heterocycles. The cytotoxic study revealed that the majority of the tested compounds possess significant anti-tumor activity towards the tested tumor cell lines.

Keywords:

Sebacoyl chloride, acid chloride, decanedihydrazide, azole, N-heterocycles, anti-tumour activity., Sebacoyl chloride, acid chloride, decanedihydrazide, azole, N-heterocycles, anti-tumour activity.

Affiliation:

Chemistry Department, Faculty of Science, Aswan University, Aswan, P.O. box 81528, Aswan, Chemistry Department, Faculty of Science, Aswan University, Aswan, P.O. box 81528, Aswan

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