Synthesis, characterisation and evaluation of oxadiazole as promising anticancer agent
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Synthesis, characterisation and evaluation of oxadiazole as promising anticancer agent S. V. Mamatha1 · S. L. Belagali1 · Mahesh Bhat2 Received: 16 December 2019 / Accepted: 12 March 2020 © Springer Nature Switzerland AG 2020
Abstract A unique series oxadiazoles were synthesized by cyclization of benzophenone hydrazide, followed by the nucleophillic alkylation of heterocyclic scaffold. Synthesized title compounds were characterized by the FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for the anticancer activity. IC50 values of the 7h observed for in-vitro anti-cancer activities were 112.6 µg/ml and 126.7 µg/ml, against the MCF-7 and KB cell lines respectively. Most active compounds were found to be less toxic, which were determined by MTT assay method with normal cell line (L292). Biological screening of the synthesized series of compounds reveals that, Compound 7h was the potent molecule.
Electronic supplementary material The online version of this article (https://doi.org/10.1007/s42452-020-2511-z) contains supplementary material, which is available to authorized users. * S. V. Mamatha, [email protected] | 1Environmental Chemistry Section, Department of Studies in Environmental Science, University of Mysore, Manasagangothri, Mysore, Karnataka 570 006, India. 2PG Department of Chemistry, JSS College for Women, Saraswathipuram, Mysore, Karnataka 570 009, India. SN Applied Sciences
(2020) 2:882
| https://doi.org/10.1007/s42452-020-2511-z
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Research Article
SN Applied Sciences
(2020) 2:882
| https://doi.org/10.1007/s42452-020-2511-z
Graphic abstract
Keywords Benzophenone · Oxadiazole · Anti-cancer · Morpholine · Piperidine
1 Introduction and experimental The recognition of prime molecular targets for cancer therapy has paved the way to a paradigm shuffle in drug discovery and thus more up thrust is now placed on molecules for drug designing. A plethora of heterocycles containing nitrogen have been the center of attention for their high therapeutic values in the past few decades. Cancer is one of the most life threatening diseases for mankind. Approximately 38.4% of men and women will be diagnosed with cancer at some point during their lifetimes and according to the World Health Organization (WHO), in 2018 globally 9.6 million deaths was due to the cancer and one in six deaths is from the cancer. When diseases become tolerant to pharmaceutical treatments this phenomenon is known as Drug resistance [1]. Multidrug resistance continues to be the principal limiting factor to achieving cures in patients with cancer. To overcome the MDR limitations many research has taken place and in that oxadiazole is one of the promising scaffold in the
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medicinal chemistry [2]. Oxadiazoles are physiologically active heterocyclic compounds owing to a vast sphere of biological activities, including anticancer [3–11], antidiabetic [12], antiviral [13, 14], anti-inflammatory [15, 16], antibacterial [17, 18], antifungal [19], antimycobacter
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