Synthesis of 2,2,4-trimethyl-1,2-dihydroquinolinyl substituted 1,2,3-triazole derivatives: Their evaluation as potential PDE 4B inhibitors possessing cytotoxic properties against cancer cells

Praveena, Koduru Sri Shanthi; Durgadas, Shylaprasad; Babu, Nallapati Suresh; Akkenapally, Surekha; Kumar, C. Ganesh; Deora, Girdhar Singh; Murthy, N. Y. S.; Mukkanti, K.; Pal, Sarbani

doi:10.1016/j.bioorg.2013.12.002

Cited by 29 publications

(6 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The standard inhibition percentage of PDE4B at 30 mM is 58.2% and also has a notable value of IC 50 ¼ 8.7 AE 0.24 towards the A549 cancer cell line. 96 The collaborative effect of quinoline, triazole, and dihydroquinoline in a single pharmacophoric group has the capability of inhibiting PDE4B and some cancer cell lines. Compound 58 is the most active against these two different cancer cell lines A549 and MCF 7.…”

Section: Introductionmentioning

confidence: 99%

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

et al. 2020

View full text Add to dashboard Cite

show abstract

Section: Introductionmentioning

confidence: 99%

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

et al. 2020

View full text Add to dashboard Cite

show abstract

“…The expression of PDE4B varied among different cancer type and its prognostic significance remains controversial in cancer (42). PDE4B expression was found to be increased in non-small cell lung cancer tissues (43), and additional study highlights in vitro findings that specific PDE4B inhibition is cytotoxic in lung cancer cells (44). IFITM1 encodes a protein that is a member of the interferon-inducible transmembrane protein family and was initially known as a leukocyte antigen, a part of the membrane complex involved in the transduction of antiproliferative and (45)(46)(47).…”

Section: Discussionmentioning

confidence: 87%

Development of an Oncogenic Driver Alteration Associated Immune-Related Prognostic Model for Stage I-II Lung Adenocarcinoma

Chen

Xie

et al. 2021

Front. Oncol.

View full text Add to dashboard Cite

Lung adenocarcinoma (LUAD) needs to be stratified for its heterogeneity. Oncogenic driver alterations such as EGFR mutation, ALK translocation, ROS1 translocation, and BRAF mutation predict response to treatment for LUAD. Since oncogenic driver alterations may modulate immune response in tumor microenvironment that may influence prognosis in LUAD, the effects of EGFR, ALK, ROS1, and BRAF alterations on tumor microenvironment remain unclear. Immune-related prognostic model associated with oncogenic driver alterations is needed. In this study, we performed the Cox-proportional Hazards Analysis based on the L1-penalized (LASSO) Analysis to establish an immune-related prognostic model (IPM) in stage I-II LUAD patients, which was based on 3 immune-related genes (PDE4B, RIPK2, and IFITM1) significantly enriched in patients without EGFR, ALK, ROS1, and BRAF alterations in The Cancer Genome Atlas (TCGA) database. Then, patients were categorized into high-risk and low-risk groups individually according to the IPM defined risk score. The predicting ability of the IPM was validated in GSE31210 and GSE26939 downloaded from the Gene Expression Omnibus (GEO) database. High-risk was significantly associated with lower overall survival (OS) rates in 3 independent stage I-II LUAD cohorts (all P < 0.05). Moreover, the IPM defined risk independently predicted OS for patients in TCGA stage I-II LUAD cohort (P = 0.011). High-risk group had significantly higher proportions of macrophages M1 and activated mast cells but lower proportions of memory B cells, resting CD4 memory T cells and resting mast cells than low-risk group (all P < 0.05). In addition, the high-risk group had a significantly lower expression of CTLA-4, PDCD1, HAVCR2, and TIGIT than the low-risk group (all P < 0.05). In summary, we established a novel IPM that could provide new biomarkers for risk stratification of stage I-II LUAD patients.

show abstract

“…The novel nimesulide-based new class of triazole derivatives 49a–d ( Figure 24 ) were synthesized as PDE4B inhibitors [ 67 ]. The synthesized compounds were tested against cancer cells, keeping in view the reported anticancer activity of nimesulide [ 68 ] and the anti-inflammatory activity of 1,2,4-triazoles [ 69 ].…”

Section: Selective Pde4b Inhibitorsmentioning

confidence: 99%

Selective Phosphodiesterase 4B Inhibitors: A Review

Azam¹

2014

Sci. Pharm.

View full text Add to dashboard Cite

Phosphodiesterase 4B (PDE4B) is a member of the phosphodiesterase family of proteins that plays a critical role in regulating intracellular levels of cyclic adenosine monophosphate (cAMP) by controlling its rate of degradation. It has been demonstrated that this isoform is involved in the orchestra of events which includes inflammation, schizophrenia, cancers, chronic obstructive pulmonary disease, contractility of the myocardium, and psoriatic arthritis. Phosphodiesterase 4B has constituted an interesting target for drug development. In recent years, a number of PDE4B inhibitors have been developed for their use as therapeutic agents. In this review, an up-to-date status of the inhibitors investigated for the inhibition of PDE4B has been given so that this rich source of structural information of presently known PDE4B inhibitors could be helpful in generating a selective and potent inhibitor of PDE4B.

show abstract

Synthesis of 2,2,4-trimethyl-1,2-dihydroquinolinyl substituted 1,2,3-triazole derivatives: Their evaluation as potential PDE 4B inhibitors possessing cytotoxic properties against cancer cells

Cited by 29 publications

References 21 publications

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

Development of an Oncogenic Driver Alteration Associated Immune-Related Prognostic Model for Stage I-II Lung Adenocarcinoma

Selective Phosphodiesterase 4B Inhibitors: A Review

Contact Info

Product

Resources

About