19207-92-2Relevant academic research and scientific papers
Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors
Abdallah, Abdallah E.,Mabrouk, Reda R.,Al Ward, Maged Mohammed Saleh,Eissa, Sally I.,Elkaeed, Eslam B.,Mehany, Ahmed B. M.,Abo-Saif, Mariam A.,El-Feky, Ola A.,Alesawy, Mohamed S.,El-Zahabi, Mohamed Ayman
, p. 573 - 591 (2022/01/20)
Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised. VEGFR-2 IC50 values ranged from 60.00 to 123.85 nM for the new derivatives compared to 54.00 nM for sorafenib. Compounds 15a, 15b, and 15d showed IC50 from 17.39 to 47.10 μM against human cancer cell lines; hepatocellular carcinoma (HepG2), prostate cancer (PC3), and breast cancer (MCF-7). Meanwhile, the first in terms of VEGFR-2 inhibition was compound 15d which came second with regard to antitumor assay with IC50 = 24.10, 40.90, and 33.40 μM against aforementioned cell lines, respectively. Furthermore, Compound 15d increased apoptosis rate of HepG2 from 1.20 to 12.46% as it significantly increased levels of Caspase-3, BAX, and P53 from 49.6274, 40.62, and 42.84 to 561.427, 395.04, and 415.027 pg/mL, respectively. Moreover, 15d showed IC50 of 253 and 381 nM against HER2 and FGFR, respectively.
A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation
Anbar, Hanan S.,El-Awady, Raafat,El-Gamal, Mohammed I.,El-Gamal, Randa,Foster, Paul A.,Potter, Barry V. L.,Zaraei, Seyed-Omar
, (2020/03/23)
Steroid sulfatase (STS) has recently emerged as a drug target for management of hormone-dependent malignancies. In the present study, a new series of twenty-one aryl amido-linked sulfamate derivatives 1a-u was designed and synthesized, based upon a cycloh
Synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors
Semreen, Mohammad H.,El-Gamal, Mohammed I.,Ullah, Saif,Jalil, Saquib,Zaib, Sumera,Anbar, Hanan S.,Lecka, Joanna,Sévigny, Jean,Iqbal, Jamshed
, p. 2741 - 2752 (2019/05/15)
A new series of sulfonate derivatives 1a–zk were synthesized and evaluated as inhibitors of nucleotide pyrophosphatases. Most of the compounds exhibited good to moderate inhibition towards NPP1, NPP2, and NPP3 isozymes. Compound 1m was a potent and selective inhibitor of NPP1 with an IC50 value of 0.387 ± 0.007 μM. However, the most potent inhibitor of NPP3 was found as 1x with an IC50 value of 0.214 ± 0.012 μM. In addition, compound 1e was the most active inhibitor of NPP2 with an IC50 value of 0.659 ± 0.007 μM. Docking studies of the most potent compounds were carried out, and the computational results supported the in vitro results.
Novel 3/4-((Substitutedbenzamidophenoxy)methyl)-N-hydroxybenzamides/propenamides and its use
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Paragraph 0101; 0103; 0104, (2020/03/17)
The present invention relates to novel 3/4-((substituted benzamidophenoxy) methyl) -N-hydroxy benzamide/propenamide, as a histone deacetylase (HDAC) inhibitor, and to an anticancer composition comprising the same as an active ingredient. More specifically
Chlorination of N-acyl derivatives of p-aminophenols (naphthols) and p-phenylenediamines
Avdeenko,Marchenko
, p. 822 - 829 (2007/10/03)
The chlorination of N-acyl derivatives of p-aminophenols can provide either N-acyl-2,3,6-trichloro-4-aminophenols or N-acyl-2,3,5,6-tetrachloro-1,4-benzoquinone imines depending on solvent nature, process temperature, and molar ratio initial compound-chlorine. The chlorination of N-acyl-4-amino-1-naphthols affords only N-acyl-2,3-dichloro-1,4-naphthoquinone imines. N,N′-Diacyl-1,4-phenylenediamines give rise on chlorination to a mixture of 2,5-dichloro-, 2,6-dichloro-, and 2,3-dichloro-N,N′-diacyl-1, 4-phenylenediamines.
Synthesis and Antiarrhythmic and Parasympatholytic Properties of Substituted Phenols. 2. Amides
Stout, David M.,Matier, W. L.,Barcelon-Yang, Cynthia,Reynolds, Robert D.,Brown, Barry S.
, p. 1347 - 1350 (2007/10/02)
Thirty amides patterned after the antiarrhythmic drug changrolin were synthesized and their antiarrhythmic and parasympatholytic activities were assessed. There was no correlation between antiarrhythmic and parasympatholytic activities. Several of the ami
