2018
DOI: 10.1002/cmdc.201800402
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Design and Synthesis of DNA‐Interactive β‐Carboline–Oxindole Hybrids as Cytotoxic and Apoptosis‐Inducing Agents

Abstract: A new series of (E)-3-[(1-aryl-9H-pyrido[3,4-b]indol-3-yl)methylene]indolin-2-one hybrids were synthesized and evaluated for their in vitro cytotoxic activity against a panel of selected human cancer cell lines, namely, HCT-15, HCT-116, A549, NCI-H460, and MCF-7, including HFL. Among the tested compounds, (E)-1-benzyl-5-bromo-3-{[1-(2,5-dimethoxyphenyl)-9H-pyrido[3,4-b]indol-3-yl]methylene}indolin-2-one (10 s) showed potent cytotoxicity against HCT-15 cancer cells with an IC value of 1.43±0.26 μm and a GI valu… Show more

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Cited by 52 publications
(29 citation statements)
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“…DAPI (4‘,6‐diamidino‐2‐phenylindole) nucleic acid staining technique is used to identify the nuclear damage or chromatin condensation. DAPI is a fluorescent dye which strongly interacts with A−T rich regions of DNA in the nucleus and stains apoptotic cells in blue . Hence, we performed the DAPI staining to detect nuclear damage by treatment of compound 11 f on HCT‐116 cells.…”
Section: Pharmacologymentioning
confidence: 99%
“…DAPI (4‘,6‐diamidino‐2‐phenylindole) nucleic acid staining technique is used to identify the nuclear damage or chromatin condensation. DAPI is a fluorescent dye which strongly interacts with A−T rich regions of DNA in the nucleus and stains apoptotic cells in blue . Hence, we performed the DAPI staining to detect nuclear damage by treatment of compound 11 f on HCT‐116 cells.…”
Section: Pharmacologymentioning
confidence: 99%
“…AO can pervade intact cell membranes and stain the nuclei green, whereas EB can only stain the nuclei of cells that have lost membrane integrity. 45 Staining images are depicted in Fig. 14.…”
Section: Molecular Docking With B-dnamentioning
confidence: 99%
“…The structural features of naturally occurring β-carboline alkaloids make it a potential chromophore to intercalate with DNA in between the base pairs. The tricyclic pyrido [3,4- b ] ring system (norharmane A ) possesses an affinity to stack between GC residues of DNA [17] . Furthermore, these Peganum harmala derived agents (harmine B ) followed up by their chemical functionalization were reported as DNA damaging and photocleavage agents [18] , (a) , (b) , (c) .…”
Section: Introductionmentioning
confidence: 99%