Abstract
Background1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β3-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. But its application is limited, as it has side effects like low bioavailability and high toxicity. Molecular docking is an exemplary tool, helps in identifying target and designing a drug containing high bio-availability and minimum toxicity.ResultsA set of 1,2,4-oxadiazole linked 5-fluoruracil derivatives (7a–j) were synthesized and their structures were confirmed by 1HNMR, 13CNMR and Mass spectral analysis. Further, these compounds were investigated for their anticancer activity towards a panel of four human cancer cell lines such as (MCF-7, MDA MB-231), lung cancer (A549) and prostate cancer (DU-145) by using MTT method. Among them, compounds 7a, 7b, 7c, 7d and 7i demonstrated more promising anticancer activity than standard.ConclusionSynthesized derivatives (7a–j) of 1,2,4-oxadiazole linked 5-fluorouracil and investigated for their anticancer activity towards a panel of four human cancer cell lines.
Highlights
Over the past few decades, heterocyclic rings containing nitrogen atoms have played a significant role in medicinal chemistry
The synthesis of 1,2,4-oxadiazole linked 5-fluorouracil derivatives (7a–j) described in this study are outlined in Scheme 1
Human cancer cell lines such as
Summary
Over the past few decades, heterocyclic rings containing nitrogen atoms have played a significant role in medicinal chemistry. Among all the nitrogenated compounds, pyrimidines are a more privileged class of six-membered heterocyclic organic units They occupy a unique position in medicinal chemistry due to their wide range of biological applications [2,3,4,5,6,7,8,9,10,11,12]. Oxadiazoles are a unique class of nitrogen and oxygen atoms containing five-membered ring heterocyclic core units [25]. They are frequently found in marine organisms [26]. The US FDA approved drug such as ataluren (2), contains 1,2,4-oxadiazole framework as a part of the structure and is used for the treatment of muscular dystrophy [37,38,39]
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