51848-56-7Relevant academic research and scientific papers
Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies
Ammazzalorso, Alessandra,Carradori, Simone,Angeli, Andrea,Akdemir, Atilla,De Filippis, Barbara,Fantacuzzi, Marialuigia,Giampietro, Letizia,Maccallini, Cristina,Amoroso, Rosa,Supuran, Claudiu T.
, p. 1051 - 1061 (2019)
A large library of fibrate-based N-acylsulphonamides was designed, synthesised, and fully characterised in order to propose them as zinc binders for the inhibition of human carbonic anhydrase (hCA) enzymatic activity. Synthesised compounds were tested aga
The critical role of novel benzophenone analogs on tumor growth inhibition targeting angiogenesis and apoptosis
Mohammed, Yasser Hussein Eissa,Ara Khanum, Shaukath
, p. 639 - 656 (2018/05/03)
In modern biology, one of the major topics of importance is progress in anti-cancer drugs with specific targets. The angiopreventive and in vitro tumor inhibition activities of novel synthetic benzophenone analogs have been investigated intensively and explored in a very systematic way. Novel benzophenone analogs (9a-d and 10a-d) substituted with methyl, chloro and fluoro groups at different positions on an identical chemical backbone and incorporating variations in the number of substituents have been synthesized in a multistep process and characterized. In this study, we further evaluate the newly synthesized compounds for their cytotoxic and anti-proliferative effects against A549, HeLa and MCF-7 cells. The potent lead compound was further assessed for anti-angiogenic effects. Through the structure-activity relationship, we found that an increase in the number of methyl, chloro and fluoro groups in a benzophenone ring on compound 9d resulted in higher potency compared to other compounds. Tumor inhibition was notably promoted, and this was reflected in effects on neovessel formation in in vivo systems, such as the CAM. Compound 9d interacts with rVEGF through hydrogen bonds in silico, thereby down-regulating the expression of VEGF in angiogenesis. From our investigation, it is suggested on the basis of clonogenesis and cell migration assays that compound 9d has the potency to exhibit prolonged activity against cancer progression, through cell cycle arrest at the G2/M phase. In addition, compound 9d inhibits A549 cells through caspase-activated DNase-mediated apoptosis.
METHODS OF IDENTIFYING CROSSLINKING MOLECULES FOR POLYMERS
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Paragraph 0112; 0113, (2015/06/03)
Methods for screening molecules or moieties for their ability to crosslink are disclosed. An aromatic carbonate, aromatic ester, or aliphatic ester group is attached to the molecule to mimic the presence of a polymer. A solution of the modified molecule i
Effect of stilbene and chalcone scaffolds incorporation in clofibric acid on PPARα agonistic activity
Giampietro, Letizia,D'Angelo, Alessandra,Giancristofaro, Antonella,Ammazzalorso, Alessandra,De Filippis, Barbara,Di Matteo, Mauro,Fantacuzzi, Marialuigia,Linciano, Pasquale,Maccallini, Cristina,Amoroso, Rosa
, p. 59 - 65 (2014/01/17)
In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, new compounds based on a combination of clofibric acid, the active metabolite of clofibrate, and trans-stilbene, chalcone, and other lipophilic groups were synthesized. They were evaluated for PPARα transactivation activity; all branched derivatives showed an increase of the transcriptional activity of receptor compared to the linear ones. Noteworthy, stilbene and benzophenone branched derivatives activated the PPARα better than clofibric acid.
Benzhydrylamine linker grafting: A strategy for the improved synthesis of C-terminal peptide amides
Alewood, Dianne,Hopping, Gene,Brust, Andreas,Reid, Robert C.,Alewood, Paul F.
experimental part, p. 551 - 557 (2011/11/12)
The standard p-MBHA resin used during Boc-chemistry synthesis of peptides carrying C-terminal carboxamides is compromised by batch-to-batch variations in its performance. This can cause artificially 'difficult' couplings during peptide chain assembly, which may ultimately lead to failed syntheses given the inability to achieve acceptable coupling yields. To overcome these problems, we have developed a new approach by grafting a functionalized benzhydrylamine linker onto well-characterized and well-performing PAM resins. We combine optimized Boc-chemistry, high-performing PAM resins and new benzhydrylamine-based linkers to achieve improved syntheses of peptide amides. Here we present the synthesis of two new benzhydrylamine linkers and their attachment to selected PAM resins. This novel solid support was evaluated through the synthesis of selected 'difficult' conotoxins and monitoring the coupling efficiency using quantitative ninhydrin assay. The results show a superior performance of the novel linker solid support compared to the standard p-MBHA resins routinely used. In summary, we describe an alternative linker-resin system that allows improved access to C-terminal amide peptides employing Boc/Bzl chemistry. Benzhydrylamine enzhydrylamine linkers (a/b) were grafted onto high-performing Phe-PAM resins for Boc solid phase peptide amide synthesis. Fast couplings with high fidelity were achieved enabling the synthesis of selected conotoxins that previously demonstrated artificially 'difficult sequences' on commercially available p-MBHA resins. Copyright
Synthesis of a thioester linker precursor for a general preparation of peptide C-terminal thioacids
Gaertner, Hubert,Villain, Matteo,Botti, Paolo,Canne, Lynne
, p. 2239 - 2241 (2007/10/03)
A general procedure to prepare peptide thioacids by solid-phase peptide synthesis is presented. The method involves the synthesis of 4-[α-(S-acetyl)mercaptobenzyl]phenoxyacetic acid as general precursor. This reagent once attached to a solid support is de
Synthesis of 5-(4′-aroyl)-aryloxy methyl-4H-(1,2,4)-triazolin-3-thiol and their biological activity
Sudha,Shashikanth,Khanum, Shaukath Ara
, p. 85 - 88 (2007/10/03)
5-(4′-aroyl)-aryloxy methyl-4H-1,2, 4)-triazolin-3-thiols were synthesized by using substituted phenyl benzoates as the starting material. Phenyl benzoates on Fries rearrangement gave p-hydroxy benzophenones which on treatment with ethyl bromoacetate in presence of anhydrous potassium carbonate and dry acetone gave corresponding benzoyl phenyloxy esters in excellent yield. Esters were refluxed with thiosemicarbazide in presence of acetic anhydride gave cyclized title compounds. Supports for the structures of the synthesized compounds have been provided by their elemental analysis and spectral data. The newly synthesized compounds were screened for antibacterial and antifungal activities.
Synthesis and antimicrobial activity of 5-[(4-aroyl) aryloxymethyl]-2-(4-methylphenylamino)-1,3,4-thiadiazoles and 5-[(4-aroyl) aryloxy methyl]-4-(4-methylphenyl)-3-mercapto-4H-1,2,4-triazoles
Sudhab,Shashikanth,Khanum, Shaukath Ara
, p. 2652 - 2656 (2007/10/03)
Aroyl aryloxyacetic thiosemicarbazides 4a-d have been synthesized by the reaction of acid hydrazides 3a-d with p-tolyl isothiocyanate. The aroyl aryloxyacetic thiosemicarbazides 4a-d on intramolecular cyclization using conc.H2SO4 and
