Synthesis of new diarylamides with pyrimidinyl pyridine scaffold and evaluation of their anti-proliferative effect on cancer cell lines

Bioorganic & Medicinal Chemistry Letters
Ahmed Z AbdelazemSo Ha Lee

Abstract

A new series of diarylamides, having a pyrimidinyl pyridine scaffold, was designed and synthesized. The target compounds were synthesized in three steps. A selected group from the target compounds was tested over a panel of 60 cancer cell lines at a single dose concentration of 10 μM, and the most active compound, 5j, was further tested in a five-dose testing mode to determine its IC50 value over the 60 cell lines. In single-dose testing mode, compound 5j showed the highest growth inhibition against the NCI-60 cancer cell lines, while other tested compounds showed a weak to moderate inhibitory activity against a range of different cancer cell lines. In five-dose testing mode, compound 5j showed strong inhibitory activity in micro molar range against many cancer cell lines. Its major activity was against melanoma cancer cell lines. Therefore, compound 5j is a promising hit compound targeting this severe form of cancer.

References

Jul 18, 2002·Nature Reviews. Drug Discovery·Renaud CapdevilleAlex Matter
Nov 8, 2006·Molecular Cancer Therapeutics·Ogechi N IkediobiRichard Wooster
May 26, 2009·Bioorganic & Medicinal Chemistry Letters·Bong Soo NamKyung Ho Yoo
Oct 28, 2009·Bioorganic & Medicinal Chemistry Letters·Myung-Ho JungChang-Hyun Oh
Nov 10, 2009·Bioorganic & Medicinal Chemistry Letters·Hee Jin KimChang-Hyun Oh
May 15, 2010·Bioorganic & Medicinal Chemistry Letters·Hana YuJung-Mi Hah
May 18, 2010·Bioorganic & Medicinal Chemistry·Ibrahim Mustafa El-Deeb, So Ha Lee
Oct 25, 2011·Nature Reviews. Cancer·Norbert BerndtSaïd M Sebti

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Citations

Jan 21, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mohammad M Al-SaneaMohamed A Abdelgawad

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