Abstract
A series of newly 1,3,4-oxadiazole-2-thioglycoside derivatives were synthesized. The key step of this protocol is the coupling between 5-herteroaryl-1,3,4-oxadiazole-2-thione and activated sugars (cyclic or acyclic sugar analogues) in the presence of basic medium. Among of the synthesized compounds, compounds 7, 10, 11 and 13 were screened for them in vitro anticancer activity against four human cancer cells. MCF-7 (Breast), HEPG2 (Liver), HCT116 (Colon) and HEP2 (Larynx) carcinoma cell lines with IC50 values ranging from 2.08 - 8.72 μg/well. Compounds 11 and 13 were highly specific and potent for four cell lines (MCF-7, HCT116, HEPG2 and HEP2).
Highlights
Among the various human diseases, cancer has proven to be one of the most intractable diseases to which humans are subjected, and as yet no practical and generally effective drugs or methods of control are available
MCF-7 (Breast), HEPG2 (Liver), HCT116 (Colon) and HEP2 (Larynx) carcinoma cell lines with IC50 values ranging from 2.08 - 8.72 μg/well
[1] identification of novel potent, selective, and less toxic anticancer agents remains one of the most pressing health problems [1]. 1,3,4-oxadiazoles are an important class of heterocyclic compounds with wide range of biological activities such as anti-inflammatory [2,3,4], anticancer in various cancer cell lines [5,6,7], antiviral [8], antimicrobial [9], antineoplastic [10], fungicidal [11], inhibition of tyrosinase [12] and cathepsin k [13]
Summary
Among the various human diseases, cancer has proven to be one of the most intractable diseases to which humans are subjected, and as yet no practical and generally effective drugs or methods of control are available. The role of the carbohydrate moiety includes enhancement of DNA sequence specificity and cell recognition [15]. Other properties augmented by carbohydrates are membrane permeability, water solubility, and chirality of chromophores or DNA damaging molecules. These characteristics suggest that introduction of carbohydrate moieties into synthetic drugs should generate hybrid molecules of considerable interest. High levels of glucosylation are one of the many molecular changes that accompany malignant transformations These changes are characteristic for cancer cells and can protect them from immune surveillance and chemotherapeutic agents, and enhance their metastatic capacity [16]. The carbohydrate moiety can be expected to play the role of drug carrier and improve the selectivity of compounds for cancerous cell lines. Vaccination using synthetic tumor associated antigens such as carbohydrate antigens, holds promise for generating a specific antitumor response by targeting the immune system to cancer cells [17]
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