24392-05-0Relevant academic research and scientific papers
Synthesis and anticancer evaluation of novel isoxazole/pyrazole derivatives
Abu Bakr, Sherifa M.,Abd El-Karim, Somaia S.,Said, Medhat M.,Youns, Mahmoud M.
, p. 1387 - 1399 (2016)
The key intermediate 3-amino-5-methylisoxazole (1) was allowed to react with phthalic anhydride and/or maleic anhydride under different conditions to produce different isoxazole products. Schiff bases 9a-c obtained via the reaction of 1 with different aldehydes were condensed with thioglycolic acid to afford the corresponding thiazolidin-4-one derivatives 10a, b. Furthermore, condensation of the Schiff bases 9a, c with various secondary amines produced the corresponding 5-substituted pyrazole derivatives 11a-d, respectively. The anticancer activity of some of the newly synthesized compounds was evaluated against Panc-1 and Caco-2 cell lines using doxorubicin as a standard drug. Most of the tested derivatives exhibited high cytotoxic potency against Panc-1 carcinoma cell lines, but moderate to weak activity was obtained against Caco-2 cell lines.
Design, synthesis and molecular docking study of novel quinoxalin-2(1H)- ones as anti-tumor active agents with inhibition of tyrosine kinase receptor and studying their cyclooxygenase-2 activity
Galal, Shadia A.,Khairat, Sarah H.M.,Ragab, Fatma A.F.,Abdelsamie, Ahmed S.,Ali, Mamdouh M.,Soliman, Salwa M.,Mortier, Jérémie,Wolber, Gerhard,El Diwani, Hoda I.
, p. 122 - 132 (2014)
On continuation to our work, new quinoxalin-2(1H)-ones were synthesized to study their cytotoxic effect against HepG-2 and MCF-7 with their effect on the human tyrosine kinase (TRK). Compounds 12, 18, 15, 13, 11a, 20 and 16, respectively, were found to be more potent than cisplatin against HepG2 and selective to TRK. Also, compounds 12, 18, 20, 13, 14, and 22, respectively, exhibited decidedly activity against MCF-7 and selectivity against human TRK compared to cisplatin. A molecular docking study was also performed to gain comprehensive understanding into plausible binding modes and to conclude the structure activity relationships of the synthesized compounds. Moreover, anti-inflammatory activity was studied. Compounds 12, 15, 18 and 22 were found to be potent and selective against COX-2.
Design, synthesis and molecular docking study of novel quinoxalin-2(1H)-ones as anti-tumor active agents with inhibition of tyrosine kinase receptor and studying their cyclooxygenase-2 activity
Galal, Shadia A.,Khairat, Sarah H.M.,Ragab, Fatma A.F.,Abdelsamie, Ahmed S.,Ali, Mamdouh M.,Soliman, Salwa M.,Mortier, Jérémie,Wolber, Gerhard,El Diwani, Hoda I.
, p. 122 - 132 (2015/02/02)
On continuation to our work, new quinoxalin-2(1H)-ones were synthesized to study their cytotoxic effect against HepG-2 and MCF-7 with their effect on the human tyrosine kinase (TRK). Compounds 12, 18, 15, 13, 11a, 20 and 16, respectively, were found to be more potent than cisplatin against HepG2 and selective to TRK. Also, compounds 12, 18, 20, 13, 14, and 22, respectively, exhibited decidedly activity against MCF- 7 and selectivity against human TRK compared to cisplatin. A molecular docking study was also performed to gain comprehensive understanding into plausible binding modes and to conclude the structure activity relationships of the synthesized compounds. Moreover, anti-inflammatory activity was studied. Compounds 12, 15, 18 and 22 were found to be potent and selective against COX-2.
