Browsing by Author "Mohammed Nissan, Yassin"

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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.
Synthesis and Anti-inflammatory Activity of Some Benzofuran and Benzopyran-4-one Derivatives
(Chemical and Pharmaceutical Bulletin, 2011) Abd El-Fattah Ragab, Fatma; Mahmoud Eid, Nahed; Sayed Hassan, Ghaneya; Mohammed Nissan, Yassin
New series of furosalicylic acids 3a—c, furosalicylanilides 6a—n, furobenzoxazines 8a—f, 1-benzofuran- 3-arylprop-2-en-1-ones 12a,b, 6-(aryl-3-oxoprop-1-enyl)-4H-chromen-4-ones 16a—c and 6-[6-aryl-2-thioxo- 2,5-dihydropyrimidin-4-yl]-4H-chromen-4-ones 17a—c were synthesized. Anti-inflammatory activity evaluation was performed using carrageenan-induced paw edema model in rats and prostaglandin E2 (PGE2) synthesis inhibition activity. Some of the tested compounds revealed comparable activity with less ulcerogenic effect than Diclofenac at a dose 100 mg/kg. All the synthesized compounds were docked on the active site of cyclooxygenase-2 (COX-2) enzyme and most of them showed good interactions with the amino acids of the active site comparable to the interactions exhibited by Diclofenac.
Synthesis and biological evaluation of new pyrazolone–pyridazine conjugates as anti-inflammatory and analgesic agents
(ELSEVIER, 2014) Abdalla Khalil, Nadia; Mohamed Ahmed, Eman; Omar Mohamed, Khaled; Mohammed Nissan, Yassin; Abo-Bakr Zaitone, Sawsan
A new series of pyrazolone–pyridazine conjugates 3 and 4a–l were synthesized and characterized by spectroscopic means and elemental analyses. All compounds were tested in vivo for their anti-inflammatory and analgesic properties against diclofenac, as reference compound. The synthesized compounds were also evaluated for their ability to inhibit the production of certain inflammatory cytokines such as TNF-α and IL-6 in serum samples. The ulcerogenic potential of the synthesized compounds was also determined. IC50 values for inhibition of COX-1 and COX-2 enzymes were investigated in vitro for the most active candidates. Molecular docking was performed on the active site of COX-2 to predict their mode of binding to the amino acids. Among the synthesized derivatives, compounds 4c and 4e showed good analgesic and anti-inflammatory activities with lower ulcer index than the reference drug