Nicotinamide-based diamides derivatives as potential cytotoxic agents: synthesis and biological evaluation

Chemistry Central Journal
Min PengShaoyong Ke

Abstract

A series of diamides derivatives containing nicotinamide unit were designed, synthesized and evaluated for their potential cytotoxic activities against human cancer cell lines. All the synthesized compounds were characterized using spectroscopic methods mainly including (1)H NMR, (13)C NMR and MS. The bio-evaluation results indicated that some of the obtained compounds (such as 4d, 4h, 4i) exhibited good to moderate cytotoxic effects on lung cancer cell lines (NCI-H460, A549, and NCI-H1975), especially, compound 4d exhibited the highly potential inhibitory activities against NCI-H460 cell line with the IC50 values of 4.07 ± 1.30 μg/mL, which might be developed as novel lead compounds for potential cytotoxic agents.

References

Dec 29, 2000·Diabetologia·M KnipUNKNOWN European Nicotinamide Diabetes Intervention Trial Group
Jun 1, 2007·Journal of Medicinal Chemistry·Bin YeMonica J Kochanny
Feb 2, 2010·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·J FerlayE Steliarova-Foucher
Mar 5, 2013·Bioorganic & Medicinal Chemistry Letters·Hye-Eun ChoiKyung-Tae Lee
Jan 9, 2014·CA: a Cancer Journal for Clinicians·Rebecca SiegelAhmedin Jemal
Mar 19, 2014·The Australasian Journal of Dermatology·Andrew C Chen, Diona L Damian
Apr 22, 2014·Bioorganic Chemistry·Maosheng WanPeifu Jiao
Jan 10, 2013·ACS Medicinal Chemistry Letters·Gerard Rosse
Dec 22, 2015·Bioorganic & Medicinal Chemistry·André JeanguenatAndrew Crossthwaite
Feb 8, 2016·Tumour Biology : the Journal of the International Society for Oncodevelopmental Biology and Medicine·Ramalingam VaikundamoorthyRajaram Rajendran
Jan 21, 2017·Advanced Science·Dandan LuoJonathan F Lovell

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Citations

Mar 16, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Tamara SiberDajana Gašo-Sokač

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Methods Mentioned

BETA
silica gel column chromatography

Software Mentioned

SPSS

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