Current Issue : April - June Volume : 2020 Issue Number : 2 Articles : 5 Articles
Condensation of 2,3-dichloropyrazine with 2-aminobenzenetellurole and 2-amino-5-methylbenzenetellurole, generated in situ by\nreduction of the corresponding ditellurides, resulted in the formation of novel 10H-pyrazino[2,3-b][1,4]benzotellurazine and its\n7-methyl derivative. The products were purified via their well-crystallized 5,5-dibromo derivatives. X-ray crystallographic analysis\nof the title compound indicates that it has a pronounced V-shape and forms hydrogen-bonded dimers. Te, N-containing\nheterocycles have the potential of offering access to supramolecular assemblies....
In this article, we report the design, synthesis, photodynamic properties, and in vitro\nevaluation of photoactivatable prodrug for the poly (ADP-ribose) polymerase 1 (PARP-1) inhibitor\nTalazoparib. In order to yield a photoactivatable, inactive prodrug, photoactivatable protecting groups\n(PPGs) were employed to mask the key pharmacophore of Talazoparib. Our study confirmed the\ngood stability and photolytic effect of prodrugs. A PARP-1 enzyme inhibition assay and PARylation\nexperiment showed that the inhibitory activity of the prodrug was reduced 380 times and more\nthan 658 times, respectively, which proved that the prodrugâ??s expected activity was lost after PPG\nprotection. In BRCA1- and BRCA2-deficient cell lines, the inhibitory activity of the compound was\nsignificantly restored after ultraviolet (UV) irradiation. The results indicate that the photoactivatable\nprodrug strategy is an interesting approach for studying PARP inhibitors. Meanwhile, the described\nphotoactivatable prodrug also provided a new biological tool for the mechanism research of PARP...
New thienyl- or chlorophenyl-substituted thiazolopyrimidine derivatives and their derived\nsugar hydrazones incorporating acyclic d-galactosyl or d-xylosyl sugar moieties in addition to their\nper-O-acetylated derivatives were synthesized. Heterocyclization of the formed sugar hydrazones\nafforded the derived acyclic nucleoside analogues possessing the 1,3,4-oxadiazoline as modified\nnucleobase via acetylation followed by the cyclization process. The cytotoxic activity of the synthesized\ncompounds was studied against human breast cancer MCF7 and MDA-MB-231 cell lines as well as\nhuman colorectal cancer HCT 116 and Caco-2 cell lines. High activities were revealed by compounds\n1, 8, 10, 11, and 13 against Caco-2 and MCF7 cells in addition to moderate activities exhibited by other\ncompounds against HCT116 or MDA-MB-231 cells������...
Nine compounds bearing pyridinyl (or piperidinyl, benzimidazolyl, benzotriazolyl) groups\nbound to an azelayl moiety through an amide bond were synthesized. The structural analogy with\nsome histone deacetylase inhibitors inspired their syntheses, seeking new selective histone deacetylase\ninhibitors (HDACi). The azelayl moiety recalls part of 9-hydroxystearic acid, a cellular lipid showing\nantiproliferative activity toward cancer cells with HDAC as a molecular target. Azelayl derivatives\nbound to a benzothiazolyl moiety further proved to be active as HDACi. The novel compounds\nwere tested on a panel of both normal and tumor cell lines. Non-specific induction of cytotoxicity\nwas observed in the normal cell line, while three of them induced a biological effect only on the\nosteosarcoma (U2OS) cell line. One of them induced a change in nuclear shape and size. Cell-cycle\nalterations are associated with post-transcriptional modification of both H2/H3 and H4 histones.\nIn line with recent studies, revealing unexpected HDAC7 function in osteoclasts, molecular docking\nstudies on the active molecules predicted their proneness to interact with HDAC7. By reducing side\neffects associated with the action of the first-generation inhibitors, the herein reported compounds,\nthus, sound promising as selective HDACi...
Identifying a pressing need for the development of more effective and selective chemotherapeutic agents, compounds belonging to different panel of 2-pyrazolines derived from vanillin were synthesized from the corresponding chalcone intermediates in formic acid, acetic acid and alcohol leading to 5-(3-methoxy-4-hydroxyphenyl)-3-(substituted phenyl)-1-formyl-4,5-dihydro-1H-pyrazoles 2a-i, 5-(3-methoxy-4-hydroxyphenyl)-3-(substituted phenyl)-1acetyl-4,5-dihydro-1H-pyrazoles 3a-i and 5-(3-methoxy-4-hydroxyphenyl)-3-(substituted phenyl)-1-hydro-4,5-dihydro-1H-pyrazoles 4a-i respectively and characterized by IR, NMR and Mass spectral data. The title compounds were evaluated for anticancer activity against MCF7 and HCT 116 human cancer cell lines by MTT assay and antimicrobial activity against bacterial and fungal strains by serial dilution technique. All the compounds exhibited weak antibacterial and some displayed good antifungal activity while, compounds with electron donating substituent’s displayed excellent anticancer activity against MCF7 cells and those with electron withdrawing substituent’s showed good activity against HCT 116 cells when compared with standard drugs. Thus, some of the title compounds were found to possess good anticancer and antifungal activity warranting further research....
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