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In Vitro Anticancer Properties of Novel Bis-Triazoles

Saleh, Maysaa M.; Abuarqoub, Duaa A.; Hammad, Alaa M.; Hossan, Md Shahadat; Ahmed, Najneen; Aslam, Nazneen; Naser, Abdallah Y.; Moody, Christopher J.; Laughton, Charles A.; Bradshaw, Tracey D.

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Maysaa M. Saleh

Duaa A. Abuarqoub

Alaa M. Hammad

Md Shahadat Hossan

Najneen Ahmed

Nazneen Aslam

Abdallah Y. Naser

Christopher J. Moody

Professor of Computational Pharmaceutical Science


Asita Elengoe


Here, we describe the anticancer activity of our novel bis-triazoles MS47 and MS49, developed previously as G-quadruplex stabilizers, focusing specifically upon the human melanoma MDA-MB-435 cell line. At the National Cancer Institute (NCI), USA, bis-triazole MS47 (NCS 778438) was evaluated against a panel of sixty human cancer cell lines, and showed selective, distinct multi-log differential patterns of activity, with GI50 and LC50 values in the sub-micromolar range against human cancer cells. MS47 showed highly selective cytotoxicity towards human melanoma, ovarian, CNS and colon cancer cell lines; in contrast, the leukemia cell lines interestingly showed resistance to MS47 cytotoxic activity. Further studies revealed the potent cell growth inhibiting properties of MS47 and MS49 against the human melanoma MDA-MB-435 cell line, as verified by MTT assays; both ligands were more potent against cancer cells than MRC-5 fetal lung fibroblasts (SI > 9). Melanoma colony formation was significantly suppressed by MS47 and MS49, and time- and dose-dependent apoptosis induction was also observed. Furthermore, MS47 significantly arrested melanoma cells at the G0/G1 cell cycle phase. While the expression levels of Hsp90 protein in melanoma cells were significantly decreased by MS49, corroborating its binding to the G4-DNA promoter of the Hsp90 gene. Both ligands failed to induce senescence in the human melanoma cells after 72 h of treatment, corroborating their weak stabilization of the telomeric G4-DNA.

Journal Article Type Article
Acceptance Date Dec 8, 2022
Online Publication Date Dec 29, 2022
Publication Date 2023-01
Deposit Date Jan 3, 2023
Publicly Available Date Jan 9, 2023
Journal Current Issues in Molecular Biology
Print ISSN 1467-3037
Electronic ISSN 1467-3045
Publisher MDPI AG
Peer Reviewed Peer Reviewed
Volume 45
Issue 1
Pages 175-196
Keywords Article, apoptosis assay, bis-triazoles, cell cycle analysis, G4-DNA, Hsp90, melanoma, NCI 60 cell line panel, senescence
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