Synthesis, antitumor evaluation, and molecular docking studies of indole–indazolyl hydrazide–hydrazone derivatives
A series of ten novel hydrazide–hydrazones linked indole and indazole moieties were designed and synthesized. All the synthesized compounds were evaluated for their cytotoxicity against four human cancer cell lines (HeLa, MDA-MB-231, MCF-7, and A549). Three of the synthesized compounds showed promis...
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Veröffentlicht in: | Monatshefte für Chemie 2017-02, Vol.148 (2), p.305-314 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | A series of ten novel hydrazide–hydrazones linked indole and indazole moieties were designed and synthesized. All the synthesized compounds were evaluated for their cytotoxicity against four human cancer cell lines (HeLa, MDA-MB-231, MCF-7, and A549). Three of the synthesized compounds showed promising cytotoxicity specifically on some of the tested cell lines with
IC
50
values ranging between 1.93 and 25.6 µM. Further, one compound was identified as a promising drug lead which showed promising cytotoxicity with
IC
50
value of 1.93 µM towards MCF-7 breast cancer cell line as compared to the standard drug doxorubicin (
IC
50
value 0.98 µM). While, all these new compounds showed no cytotoxicity on the normal human embryonic kidney cell line, HEK-293.
Graphical abstract |
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ISSN: | 0026-9247 1434-4475 |
DOI: | 10.1007/s00706-016-1750-6 |