Synthesis and Spectral Studies of Novel 3-(5-mercapto-1, 3, 4-oxadiazol-2-yl)-2H-chromen-2-one Derivatives as Anticancer Agents

Chamandeep Kaur Bhinder^1*, Amandeep Kaur^2
1Department of Pharmaceutical Chemistry, ASBASJSM COP, Bela, Punjab-140111, India
²Department of Pharmaceutical Chemistry, ASBASJSM COP, Bela, Punjab-140111, India

A B S T R A C T
In recent years, researchers hunt for a novel anticancer agent mainly from plants. Among various phytochemicals, coumarins have attracted considerable interest in the past few years due to their potential health benefits. Similarly Oxadiazole is a versatile heterocyclic nucleus which has attracted a wide attention of the medicinal chemists in search for new therapeutic molecules. A series of new of 3-(5-mercapto-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one 4 derivatives were synthesized by reacting  it with some alkylating agents. The ethyl 2-oxo-2H-chromene-3-carboxylate 2 was synthesized in good yield by reacting 2-hydroxybenzaldehyde and diethyl malonate in presence of piperidine and AcOH. The 2-oxo-2H-chromene-3-carbohydrazide 3 was synthesized by refluxing 2 in presence of hydrazine hydrate 99% in ethanol. The 3-(5-mercapto-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one 4 was synthesized by refluxing 3 in presence of CS₂/KOH till evolution of H₂S ceased. This 3-(5-mercapto-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one 4 was further refluxed in presence of base and alkalyting agents to get different derivatives (WJ 1-10). By the anticancer screening we have observed that the derivatives have shown significant activity against Human leukemia Cancer (HL60) cell line, good to moderate activity against Human Breast Cancer (MCF7) cell line and moderate activity against Human Cervix Cancer (HeLa) cell line.
Keywords: cancer, coumarin, oxadiazole, leukemia, breast, cervix.