Novel 3-(3, 5-difluoro-4-hydroxyphenyl)-1-(naphthalen-2-yl) prop-2-en-1-one as a potent inhibitor of MAP-kinase in HeLa cell lines and anti-angiogenic activity is mediated by HIF-1α in EAC animal model

Guruswamy, Dileep Kumar M.; Balaji, Kyathegowdana Doddi Srivinavasa; Dharmappa, K.K.; Jayarama, Shankar

doi:10.18632/oncotarget.27836

Cited by 9 publications

(3 citation statements)

References 61 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Recently, Park et al [ 136 ] revealed the ability of LiA to inhibit the hypoxia-induced activation of HIF-1α and the subsequent down-regulation of HIF-1α-related genes. The ability to suppress HIF-1α signaling has also been documented in both synthetic and natural chalcones [ 137 , 138 , 139 ].…”

Section: Molecular and Cellular Mechanisms Of Actionmentioning

confidence: 99%

Chalcones and Gastrointestinal Cancers: Experimental Evidence

Michalková

Kello

Čižmáriková

et al. 2023

IJMS

View full text Add to dashboard Cite

Colorectal (CRC) and gastric cancers (GC) are the most common digestive tract cancers with a high incidence rate worldwide. The current treatment including surgery, chemotherapy or radiotherapy has several limitations such as drug toxicity, cancer recurrence or drug resistance and thus it is a great challenge to discover an effective and safe therapy for CRC and GC. In the last decade, numerous phytochemicals and their synthetic analogs have attracted attention due to their anticancer effect and low organ toxicity. Chalcones, plant-derived polyphenols, received marked attention due to their biological activities as well as for relatively easy structural manipulation and synthesis of new chalcone derivatives. In this study, we discuss the mechanisms by which chalcones in both in vitro and in vivo conditions suppress cancer cell proliferation or cancer formation.

show abstract

Section: Molecular and Cellular Mechanisms Of Actionmentioning

confidence: 99%

Chalcones and Gastrointestinal Cancers: Experimental Evidence

Michalková

Kello

Čižmáriková

et al. 2023

IJMS

View full text Add to dashboard Cite

show abstract

“…Naphthalene-based chalcone 18 (Figure 4) was synthesized by Guruswamy et al and analyzed its antiproliferative activity on cancer cell lines (HT29, HeLa, HCT116, MCF-7, MDA-MB-231, and SKBR3). [61] Compound 18 demonstrated exceptional anticancer activity on HeLa cell lines, as evidenced by the estimated IC 50 range of 5.58-11.13 μM. Additionally, it was shown that 18 increased Caspase 3 activation by regulating the Bax and Bcl-2 genes, which in turn triggered the mitochondrial apoptotic pathway.…”

Section: Anticancer Agentsmentioning

confidence: 96%

Naphthyl‐Based Chalcone Derivatives: A Multifaceted Player in Medicinal Chemistry

Mahesha,

Shetty

2024

ChemistrySelect

View full text Add to dashboard Cite

Research has placed a great deal of emphasis on molecule development and discovery with substantial biological profiling in recent years. Despite the significant side effects, medicinal chemists have long strived to synthesize drug molecules with the highest level of therapeutic activity and the lowest possible level of toxicity. The naphthyl‐based chalcone derivatives have drawn attention due to their simple structures and wide range of pharmacological effects. The main focus of this review is to outline the biologically active molecules based on naphthyl moiety‐substituted chalcone derivatives developed over the years. A synopsis of pharmacological screening, including relevant structure‐activity relationships, action mechanisms, and possible therapeutic applications, is provided in this article. It is true that prospective hybrids combining the naphthyl moiety with different chalcone pharmacophores are needed to address drug resistance and improve specificity. Therefore, this review may be useful in the development and design of new, highly successful therapeutic drugs based on previously reported methodologies.

show abstract

“…Developed countries are experiencing an alarming increase in cancer-related mortality rates, with approximately 10 million deaths recorded in 2020. Predictions suggest that this number will rise to 16.3 million by 2040 [ 2 , 3 ].…”

Section: Introductionmentioning

confidence: 99%

Novel quinazolines bearing 1,3,4-thiadiazole-aryl urea derivative as anticancer agents: design, synthesis, molecular docking, DFT and bioactivity evaluations

Masoudinia,

Samadizadeh,

Safavi

et al. 2024

BMC Chemistry

View full text Add to dashboard Cite

A novel series of 1-(5-((6-nitroquinazoline-4-yl)thio)-1,3,4-thiadiazol-2-yl)-3-phenylurea derivatives 8 were designed and synthesized to evaluate their cytotoxic potencies. The structures of these obtained compounds were thoroughly characterized by IR, 1H, and 13C NMR, MASS spectroscopy and elemental analysis methods. Additionally, their in vitro anticancer activities were investigated using the MTT assay against A549 (human lung cancer), MDA-MB231 (human triple-negative breast cancer), and MCF7 (human hormone-dependent breast cancer). Etoposide was used as a reference marketed drug for comparison. Among the compounds tested, compounds 8b and 8c demonstrated acceptable antiproliferative activity, particularly against MCF7 cells. Considering the potential VEGFR-2 inhibitor potency of these compounds, a molecular docking study was performed for the most potent compound, 8c, to determine its probable interactions. Furthermore, computational investigations, including molecular dynamics, frontier molecular orbital analysis, Fukui reactivity descriptor, electrostatic potential surface, and in silico ADME evaluation for all compounds were performed to illustrate the structure–activity relationship (SAR).

show abstract

Novel 3-(3, 5-difluoro-4-hydroxyphenyl)-1-(naphthalen-2-yl) prop-2-en-1-one as a potent inhibitor of MAP-kinase in HeLa cell lines and anti-angiogenic activity is mediated by HIF-1α in EAC animal model

Cited by 9 publications

References 61 publications

Chalcones and Gastrointestinal Cancers: Experimental Evidence

Chalcones and Gastrointestinal Cancers: Experimental Evidence

Naphthyl‐Based Chalcone Derivatives: A Multifaceted Player in Medicinal Chemistry

Novel quinazolines bearing 1,3,4-thiadiazole-aryl urea derivative as anticancer agents: design, synthesis, molecular docking, DFT and bioactivity evaluations

Contact Info

Product

Resources

About