Novel α-Cyano-Indolyl Chalcones as Anti-Cancer Candidates, Induce G1/S Cell Cycle Arrest and Sequentially Activate
            <i>Caspases-7, 8</i>
            , and
            <i>9</i>
            in Breast Carcinoma

Kashmiry, Alaa A.; Ibrahim, Nada S.; Mohamed, Magda F.; Abdelhamid, Ismail A.

doi:10.1080/10406638.2024.2412818

Polycyclic Aromatic Compounds

2024

DOI: 10.1080/10406638.2024.2412818

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Novel α-Cyano-Indolyl Chalcones as Anti-Cancer Candidates, Induce G1/S Cell Cycle Arrest and Sequentially Activate Caspases-7, 8 , and 9 in Breast Carcinoma

Alaa A. Kashmiry,

Nada S. Ibrahim,

Magda F. Mohamed

et al.

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Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

Abdelaal,

Ragheb,

Hassaneen

et al. 2024

Sci Rep

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A novel series of six [1,2,4]triazolo[3,4- a ]isoquinolin-3-yl)-3-(1,3-diphenyl-1 H -pyrazol-4-yl)prop-2-en-1-ones ( 3a – 3f ) was designed and synthesized. They were characterized based on spectral and elemental analyses. In silico studies were also committed to provide insights and a better understanding of their structural features. The six compounds were screened for their antiproliferative activity using the MTT assay against five human cancer cell lines, namely, A549, HCT116, PC3, HT29, and MCF-7 in parallel with the non-cancerous human lung cell line WI-38. The results showed that 3e and 3f have potential cytotoxic activities, especially on A549 cells with IC 50 = 2.3 µM and 1.15 µM, respectively. Meanwhile, they recorded a minimal cytotoxic effect on WI-38 cells. Concerning the molecular mechanism of action, the present study showed the inhibitory effect of the six compounds against total EGFR. The most potent EGFR inhibitors were 3e and 3f with IC 50 = 0.031 µM and 0.023 µM, respectively. The selectivity index of 3f for EGFR T790M was 1.81 times more selective than that of lapatinib. In addition, 3e and 3f initiated cell cycle arrest at the G2/M and pre-G1 phases along with the downregulation of anti-apoptotic protein Bcl2 and the upregulation of pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. Further studies are recommended to evaluate animal models’ promising anticancer activity and molecular mechanism of triazolo[3,4- a ]isoquinoline derivatives 3e and 3f . Supplementary Information The online version contains supplementary material available at 10.1038/s41598-024-76459-x.

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Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

Abdelaal,

Ragheb,

Hassaneen

et al. 2024

Sci Rep

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show abstract

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Novel α-Cyano-Indolyl Chalcones as Anti-Cancer Candidates, Induce G1/S Cell Cycle Arrest and Sequentially Activate Caspases-7, 8 , and 9 in Breast Carcinoma

Cited by 1 publication

References 65 publications

Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

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