13143-03-8Relevant articles and documents
Synthesis, molecular docking, and biological activities of new cyanopyridine derivatives containing phenylurea
Gezegen, Hayreddin,Gürdere, Meliha B.,Din?er, Ay?egül,?zbek, O?uz,Ko?yi?it, ümit M.,Taslimi, Parham,Tüzün, Burak,Budak, Yakup,Ceylan, Mustafa
, (2020/12/13)
A new class of cyanopyridine derivatives (10a–e and 11a–e) containing the phenylurea unit was synthesized and tested against some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase (α-Gly). The new cya
Synthesis and biological evaluation of some novel thiobenzimidazole derivatives as anti-renal cancer agents through inhibition of c-MET kinase
Ibrahim, Hany S.,Albakri, Mohamed E.,Mahmoud, Walaa R.,Allam, Heba Abdelrasheed,Reda, Ahmed M.,Abdel-Aziz, Hatem A.
, p. 337 - 348 (2019/01/18)
Benzimidazole is an interesting scaffold constituting a main core in many anticancer agents against variable cell lines as Carbendazim (I) and Nocodazole (II). Accordingly, eighteen compounds of 2-((1H-benzoimidazol-2-yl)thio)-1-(aryl/heteroaryl)ethan-1-ones, in their sulfate salt and free forms, were designed and investigated as anticancer agents. In vitro preliminary screening of selected compounds by the National Cancer Institute (NCI) on a panel of 60 cell lines revealed renal cancer cell line (A498) as the most vulnerable cell line; accordingly, IC50 values against A498 cell line were determined for compounds with the best results. The best inhibitory activity was for compound 4a with (IC50 = 6.97 μM) compared to sunitinib as a reference drug (IC50 = 6.99 μM). Compound 4a was further subjected to cell cycle analysis that indicated the decrease in cell population in the G2/M phase when compared to the untreated control cells. In addition, it showed significant increase in the late apoptosis in Annexin-V FTIC study compared to the control cells. An enzymatic inhibitory study on compound 4a against c-Met and MAP kinases revealed its better activity against c-Met kinase with (IC50 = 0.27 μM) compared to sunitinib (IC50 = 0.18 μM). Molecular docking study was conducted to reveal the interactions of compound 4a in the active site of c-Met kinase. Computational ADME study was performed to insure that compound 4a has proper pharmacokinetic and drug-likeness properties.
Synthesis and Biological Evaluation of Novel 1-(4-(Hydroxy(1-oxo-1,3-dihydro-2H-inden-2-ylidene)methyl)phenyl)-3-phenylurea Derivatives
Gezegen, Hayreddin,Hepokur, Ceylan,Tutar, U?ur,Ceylan, Mustafa
, (2017/10/24)
A series of novel phenylurea containing 2-benzoylindan-1-one derivatives 3a?–?3j were synthesized from the reaction of phenylurea-substituted acetophenones 1a?–?1j with phthalaldehyde 2 under mild reaction conditions in good yields. All synthesized compou