Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4′,3′:4,5]thieno[2,3- d ]pyrimidin-4(3 H )-one schiff bases

Narender, M.; Jaswanth, S Bhandaru; Kulandaivelu, Umasankar; Malathi, Jambulingam; Reddy, Adidala Raghuram; Umadevi, K. R.; Dusthackeer, Azger; Rao, K. Venkat; Raghuram, R Akkinepally

doi:10.1016/j.bmcl.2015.12.083

Cited by 19 publications

(3 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…PBTZ169 has one of the most minimal MICs against M. tuberculosis (0.6 nM) and came out because of a lead optimisation process. PBTZ169 has finished phase I clinical trials and acts in cooperative energy with pyrazinamide and bedaquiline [ 25 ]. DprE1 has similarly been distinguished as the objective of the dinitrobenzamides (DNBs), nitroquinoxalines (with the lead atom VI-9376) and nitroimidazoles (with the lead particle 377790), all of which act as covalent inhibitors.…”

Section: Current Status Of Dpre1 Inhibitorsmentioning

confidence: 99%

Decaprenyl-phosphoryl-ribose 2′-epimerase (DprE1): challenging target for antitubercular drug discovery

Gawad

Bonde

2018

Chemistry Central Journal

View full text Add to dashboard Cite

Tuberculosis has proved harmful to the entire history of mankind from past several decades. Decaprenyl-phosphoryl-ribose 2′-epimerase (DprE1) is a recent target which was identified in 2009 but unfortunately it is neither explored nor crossed phase II. In past several decades few targets were identified for effective antitubercular drug discovery. Resistance is the major problem for effective antitubercular drug discovery. Arabinose is constituent of mycobacterium cell wall. Biosynthesis of arabinose is FAD dependant two step epimerisation reaction which is catalysed by DprE1 and DprE2 flavoprotein enzymes. The current review is mainly emphases on DprE1 as a perspective challenge for further research.

show abstract

Section: Current Status Of Dpre1 Inhibitorsmentioning

confidence: 99%

Decaprenyl-phosphoryl-ribose 2′-epimerase (DprE1): challenging target for antitubercular drug discovery

Gawad

Bonde

2018

Chemistry Central Journal

View full text Add to dashboard Cite

show abstract

“…The promodel module was used for the active site prediction. One hundred een already known M. tuberculosis PanC inhibitors [38][39][40][41][42] were used for the docking studies ( Table 1).…”

Section: Molecular Dockingmentioning

confidence: 99%

Molecular docking, pharmacophore based virtual screening and molecular dynamics studies towards the identification of potential leads for the management of H. pylori

Damale¹,

Patil

Ansari

et al. 2019

RSC Adv.

View full text Add to dashboard Cite

show abstract

“…In fact, thieno[2,3- d ]pyrimidines with different substituted groups have been prepared and evaluated with regard to pharmaceutical functions, such as 17 beta-hydroxysteroid dehydrogenase inhibition, SIRT2 inhibition, and antimycobacterial and anti-cancer agent effects (Figure 1), etc. [13,14,15,16,17,18,19,20].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Novel Analogs of Thieno[2,3-d] Pyrimidin-4(3H)-ones as Selective Inhibitors of Cancer Cell Growth

et al. 2019

View full text Add to dashboard Cite

New 2,3-disubstituted thieno[2,3-d]pyrimidin-4(3H)-ones were synthesized via a one-pot reaction from 2H-thieno[2,3-d] [1,3]oxazine-2,4(1H)-diones, aromatic aldehydes, and benzylamine or 4-hydroxylbezylamine. The obtained compounds were tested in vitro for cancer cell growth inhibition. Compound 19 can inhibit all four types of tested cancer cells, i.e., MCF-7, A549, PC-9, and PC-3 cells. Most of the compounds inhibited the proliferation of A549 and MCF-7 cells. Compound 15 exhibited the strongest anti-proliferative effect against A549 cell lines with IC50 values of 0.94 μM, and with no toxicity to normal human liver cells. Its potency was further proved by cell clone formation assay, Hoechst 33258 staining, and evaluation on the effects of apoptosis-related proteins.

show abstract

Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4′,3′:4,5]thieno[2,3- d ]pyrimidin-4(3 H )-one schiff bases

Cited by 19 publications

References 23 publications

Decaprenyl-phosphoryl-ribose 2′-epimerase (DprE1): challenging target for antitubercular drug discovery

Decaprenyl-phosphoryl-ribose 2′-epimerase (DprE1): challenging target for antitubercular drug discovery

Molecular docking, pharmacophore based virtual screening and molecular dynamics studies towards the identification of potential leads for the management of H. pylori

Synthesis of Novel Analogs of Thieno[2,3-d] Pyrimidin-4(3H)-ones as Selective Inhibitors of Cancer Cell Growth

Contact Info

Product

Resources

About