Browsing by Author "Sulaiman Al-Said, Mansour"

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Dapson in Heterocyclic Chemistry, Part V: Synthesis, Molecular Docking and Anticancer Activity of Some Novel Sulfonylbiscompounds Carrying Biologically Active Dihydropyridine, Dihydroisoquinoline, 1,3-Dithiolan, 1,3-Dithian, Acrylamide, Pyrazole, Pyrazolopyrimidine and Benzochromenemoieties
(Chemical and Pharmaceutical Bulletin, 2012) Mohammed Ghorab, Mostafa; Sulaiman Al-Said, Mansour; Mohammed Nissan, Yassin
N,N′-(4,4′-Sulfonylbis(4,1-phenylene))bis(2-cyanoacetamid) 2 was utilized as a key intermediate for the synthesis of novel dihydropyridines 3, 4, 8, dihydroisoquinolines 5–7, dithiolan 10, dithian 11, acrylamide 12, benzochromenes 17 and 18 and chromenopyridones 19 and 20. Compound 2 was the starting material in the synthesis of the acrylamide derivative 14, the pyrazole derivative 15 and the pyrazolopyrimidine derivative 16. All the synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Compound 19 showed the best cytotoxic activity with IC50 value 19.36 μM. In addition, molecular docking study of the synthesized compounds on the active sites of farnesyltransferase and arginine methyltransferase was performed in order to give a suggestion about the mechanism of action of their cytotoxic activity.
Discovering Some Novel 7-Chloroquinolines Carrying a Biologically Active Benzenesulfonamide Moiety as a New Class of Anticancer Agents
(Chemical and Pharmaceutical Bulletin, 2013) Salem Al-Dosari, Mohammed; Mohamed Ghorab, Mostafa; Sulaiman Al-Said, Mansour; Mohammed Nissan, Yassin
Based on the reported anticancer activity of quinolines, a new series of 7-chloroquinoline derivatives bearing the biologically active benzenesulfonamide moiety 2–17 and 19–25 were synthesized starting with 4,7-dichloroquinolne 1. Compound 17 was the most active compound with IC50 value 64.41, 75.05 and 30.71 μm compared with Doxorubicin as reference drug with IC50 values 82.53, 88.32 and 73.72 μm on breast cancer cells, skin cancer cells and neuroblastoma, respectively. All the synthesized compounds were evaluated for their in vitro anticancer activity on breast cancer cells, skin cancer cells and neuroblastoma cells. Most of the synthesized compounds showed moderate activity. In order to suggest the mechanism of action for their cytotoxic activity, molecular docking for all synthesized compounds was done on the active site of phosphoinositide kinase (PI3K) and good results were obtained.