Design, synthesis, characterization, and cytotoxicity activity evaluation of mono-chalcones and new pyrazolines derivatives

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dc.contributor.authorSalum, Kassim Alien_US
dc.contributor.authorAlidmat, Mohammad Murwihen_US
dc.contributor.authorKhairulddean, Melatien_US
dc.contributor.authorKamal, Nik Nur Syazni Nik Mohammaden_US
dc.contributor.authorMuhammad, Musthahimahen_US
dc.date.accessioned2020-10-16T08:56:39Z
dc.date.available2020-10-16T08:56:39Z
dc.date.issued2020-08
dc.description.abstractThe development of resistance and side effects of chemotherapeutic drugs are common obstacles in the treatmentof cancer. With the expansion of health problems nowadays, there is a need to continuously develop new drugs thatare more efficient in targeting tumor cells and safe to normal cells. This study designed a series of new chalconesand pyrazoline derivatives based on their binding energy from the molecular docking study. The synthesis involvedClaisen–Schmidt condensation to form two chalcones, 1 and 2, which are then cyclized at room temperature to formeight new pyrazoline derivatives, 3–10. A one-pot reaction of acetophenone, 2-ethoxybenzaldehyde, and hydrazidederivatives (thiosemicarbazide and phenyl hydrazide) under reflux formed two new pyrazoline derivatives, 11 and12, without the isolation of chalcones. All the synthesized chalcones and pyrazolines were characterized using theFourier transform infrared spectroscopy–attenuated total reflectance and nuclear magnetic resonance (1D and 2D).The cytotoxicity activity of the chalcones and new pyrazoline compounds were investigated against breast cancercell lines (MCF-7 and MD-MB-231) and normal breast cell lines (MCF-10A). The results show that only compound7 showed the minimum inhibition against MCF-7 with IC50 6.50µM when exposed to the cell line for 24 hourscompared to the reference Gefitinib anticancer drugen_US
dc.identifier.affiliationsSchool of Chemical Sciences, Universiti Sains Malaysia, 11800 Penang, Malaysia.en_US
dc.identifier.affiliationsDepartment of Natural Science, The State University of Zanzibar, Zanzibar, Tanzaniaen_US
dc.identifier.affiliationsSchool of Chemical Sciences, Universiti Sains Malaysia, 11800 Penang, Malaysiaen_US
dc.identifier.affiliationsSchool of Chemical Sciences, Universiti Sains Malaysia, 11800 Penang, Malaysiaen_US
dc.identifier.affiliationsSchool of Chemical Sciences, Universiti Sains Malaysia, 11800 Penang, Malaysiaen_US
dc.identifier.affiliationsAdvanced Medical and Dental Institute, Universiti Sains Malaysia, 13200 Kepala Batas, Penang, Malaysiaen_US
dc.identifier.affiliationsAdvanced Medical and Dental Institute, Universiti Sains Malaysia, 13200 Kepala Batas, Penang, Malaysiaen_US
dc.identifier.citationSalum Kassim Ali, Alidmat Mohammad Murwih, Khairulddean Melati, Kamal Nik Nur Syazni Nik Mohammad, Muhammad Musthahimah. Design, synthesis, characterization, and cytotoxicity activity evaluation of mono-chalcones and new pyrazolines derivatives. Journal of Applied Pharmaceutical Science. 2020 Aug; 2020 Aug: 020-036en_US
dc.identifier.issn2231-3354
dc.identifier.placeIndiaen_US
dc.identifier.urihttps://imsear.searo.who.int/handle/123456789/210639
dc.languageenen_US
dc.publisherOpen Science Publishers LLPen_US
dc.relation.issuenumber8en_US
dc.relation.volume10en_US
dc.source.urihttps://dx.doi.org//10.7324/JAPS.2020.10803en_US
dc.subjectChalconeen_US
dc.subjectpyrazolineen_US
dc.subjectclaisen–schmidt condensationen_US
dc.subjectacetophenone.en_US
dc.titleDesign, synthesis, characterization, and cytotoxicity activity evaluation of mono-chalcones and new pyrazolines derivativesen_US
dc.typeJournal Articleen_US
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