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11.
Synthesis of novel 6-isocyano-5-substitutedphenyl-[1, 2, 4]
triazolopyrimidin-7(8H)-onederivatives and evaluation of their
anticancer activity
N. Kumara*, N. Singhalb, R.
Dudhea
aDepartment
of Pharmacy, Galgotias University, Greater Noida,- 201306, U. P.,
India. Mob. 9717893319, 9310497960, Email: nitinvermakr@gmail.com
bDepartment of Pharmaceutical Technology, Meerut
Institute of Engineering and Technology, Meerut-250005, U. P.,
India.Tel.: +91-1212439019, Fax: +91-1212439058
Abstract:
Two novel series of
6-isocyano-5-substitutedphenyl-[1,2,4]triazolo[4,3-a]pyrimidin-7(8H)-one
(IVa-e and Va-e) were synthesized by the reaction of aromatic
aldehyde, ethylcyanoacetate and thiourea. Synthesized compounds
were authenticated by TLC, 1HNMR, IR, MASS spectral
data and Elemental analysis. Synthesized compounds were sent to
NCIfor anti-cancer screening on 60 different cancer cell lines.
The synthesized compound of triazole derivatives IVb, IVc, Vb,
Vc and Ve having 2,4-di-OCH3, 4-F and 2,4-di-Cl
substitution exhibit good anticancer activity against the
different cancer cell lines like Leukemia cancer (K-562),CNS
cancer (SNB-75, SF-295) Renal cancer (UO-31) cell lines,
compound Vc (6-isocyano-3,
8-dimethyl-5-(4-fluorophenyl)-[1,2,4]triazolo[4,3-a]pyrimidin-7(8H)-one)
showed extremely good activity against the Leukemia cancer cell
line K-562.
Keywords:Triazole,
Anticancer, CNS cancer, Renal cancer, Leukemia cancer.
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