88-95-9Relevant articles and documents
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Greene
, p. 1503,1506 (1959)
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Design, synthesis and molecular docking studies of novel cyclic pentapeptides based on phthaloyl chloride with expected anticancer activity
Mohamed, Fatma H.,Shalaby, Ahmad M.,Soliman, Hanan A.,Abdelazem, Ahmed Z.,Mounier, Marwa M.,Nossier, Eman S.,Moustafa, Gaber O.
, p. 1723 - 1736 (2020/09/01)
Aseries of Nα-phthaloyl bridged cyclic pentapeptide derivatives were synthesized and characterized on the basis of spectral and elemental analyses. A preliminary cytotoxicity evaluation of all novel compounds was carried out against four human cancer cell lines, human lung (A-549), colon (CaCo-2), prostate (PC-3) and breast (MCF-7) cancer cells at 100 μM concentration using MTT growth inhibition assay. Compound 3 gave the highest cytotoxic activity towards the human colon (CaCo-2) cancer cell line (Growth Inhibition = 72.4 %). Further molecular docking of the promising derivative 3 was developed to study its binding mode within the active site of EGFR enzyme. The docking results suggest good fitting through different hydrogen bond interactions with the protein residues to elicit anticancer activity.
Novel bivalent securinine mimetics as topoisomerase I inhibitors
Hou, Wen,Lin, Hui,Wang, Zhen-Ya,Banwell, Martin G.,Zeng, Ting,Sun, Ping-Hua,Lin, Jing,Chen, Wei-Min
, p. 320 - 328 (2017/03/08)
A series of novel bivalent securinine mimetics incorporating different linkers between C-15 and C-15′ were synthesized and their topoisomerase I (Topo I) inhibitory activities evaluated. It was thus revealed that mimetic R2 incorporating a rigid m-substituted benzene linker exhibits Topo I inhibitory activity three times that of parent securinine. Comprehensive structure-activity relationship analyses in combination with docking studies were used to rationalize the potent activity of these bivalent mimetics. Mechanistic studies served to confirm the deductions arising from docking studies that the active bivalent mimetics not only inhibited complexation between Topo I and DNA but also stabilized the Topo I-DNA complex itself.