Non-small cell lung cancer sensitisation to platinum chemotherapy via new thiazole-triazole hybrids acting as dual T-type CCB/MMP-9 inhibitors

Gamal, Hassan; Ismail, Khadiga A.; Omar, A-Mohsen M. E.; Teleb, Mohamed; Abu-Serie, Marwa M.; Huang, Sun; Abdelsattar, Abdalla S.; Zamponi, Gerald W.; Fahmy, Hesham

doi:10.1080/14756366.2024.2388209

Journal of Enzyme Inhibition and Medicinal Chemistry

2024

DOI: 10.1080/14756366.2024.2388209

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Non-small cell lung cancer sensitisation to platinum chemotherapy via new thiazole-triazole hybrids acting as dual T-type CCB/MMP-9 inhibitors

Hassan Gamal,

Khadiga A. Ismail,

A-Mohsen M. E. Omar

et al.

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Structure optimization and molecular dynamics studies of new tumor-selective s -triazines targeting DNA and MMP-10/13 for halting colorectal and secondary liver cancers

Morcos,

Haiba,

Bassily

et al. 2024

Journal of Enzyme Inhibition and Medicinal Chemistry

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A series of triazole-tethered triazines bearing pharmacophoric features of DNA-targeting agents and non-hydroxamate MMPs inhibitors were synthesized and screened against HCT-116, Caco-2 cells, and normal colonocytes by MTT assay. 7a and 7g surpassed doxorubicin against HCT-116 cells regarding potency (IC 50 = 0.87 and 1.41 nM) and safety (SI = 181.93 and 54.41). 7g was potent against liver cancer (HepG-2; IC 50 = 65.08 nM), the main metastatic site of CRC with correlation to MMP-13 expression. Both derivatives induced DNA damage at 2.67 and 1.87 nM, disrupted HCT-116 cell cycle and triggered apoptosis by 33.17% compared to doxorubicin (DNA damage at 0.76 nM and 40.21% apoptosis induction). 7g surpassed NNGH against MMP-10 (IC 50 = 0.205 μM) and MMP-13 (IC 50 = 0.275 μM) and downregulated HCT-116 VEGF related to CRC progression by 38%. Docking and MDs simulated ligands-receptors binding modes and highlighted SAR. Their ADMET profiles, drug-likeness and possible off-targets were computationally predicted.

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Structure optimization and molecular dynamics studies of new tumor-selective s -triazines targeting DNA and MMP-10/13 for halting colorectal and secondary liver cancers

Morcos,

Haiba,

Bassily

et al. 2024

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

show abstract

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Non-small cell lung cancer sensitisation to platinum chemotherapy via new thiazole-triazole hybrids acting as dual T-type CCB/MMP-9 inhibitors

Cited by 1 publication

References 98 publications

Structure optimization and molecular dynamics studies of new tumor-selective s -triazines targeting DNA and MMP-10/13 for halting colorectal and secondary liver cancers

Structure optimization and molecular dynamics studies of new tumor-selective s -triazines targeting DNA and MMP-10/13 for halting colorectal and secondary liver cancers

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