Thiazole Containing Nitrogen Mustards: Synthesis, Structural Evaluation, Cytotoxicity and DNA Binding Studies

Raghavendra, Narasimha; Renuka, Surampudi; Gupta, Sayan Dutta; Pingili, Divya

doi:10.2174/157018011797200830

Cited by 5 publications

(2 citation statements)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Cells were incubated for 3 hours at 37 °C until intracellular purple formazan crystals are visible under microscope. Removed MTT reagent and added 100 μL of the DMSO to each well and mixed gently on an orbital shaker for one hour at room temperature. The volume of DMSO should be adjusted depending on the volume of cell culture. Measured the absorbance at OD570 nm for each well on an absorbance plate reader [22] …”

Section: Methodsmentioning

confidence: 99%

See 1 more Smart Citation

Discovery of Novel 1,2,4‐Oxadiazolyl Triazole Hybrids as B‐Raf Inhibitors for the Treatment of Melanoma

Pingili¹,

Svum²,

Raghavendra

2022

ChemistrySelect

View full text Add to dashboard Cite

A fascinating oncology target is the serine/threonine-specific protein kinase B-Raf, which is a component of the MAPK pathway. A new series of triazolo oxadiazole derivatives have been identified as the primary scaffold of small molecule B-Raf inhibitors. Twelve derivatives (7a-l) of triazolo oxadiazole hybrids were synthesized and characterized by spectral data. The evaluation of physicochemical and pharmacokinetic parameters demonstrated that the compounds' solubility, lipophilicity, and compliance with Lipinski's rule are all within acceptable ranges. The anti-proliferative capability of the synthesized derivatives was evaluated by screening them against the human melanoma cell lines Skmel-23 and A375, which express B-Raf in their wild-type and mutant forms, respectively. The IC 50 values differed significantly from those of the conventional doxorubicin. The IC 50 values for compounds 7b and 7e against Skmel-23 were determined to be 26.95 and 76.17 μM, respectively. The compounds 7b and 7c inhibited A375 cells at IC 50 concentrations of 16.64 and 78.1 μM, respectively. Therefore, these compounds were subjected to morphological screening to detect changes in cell morphology and evaluate their apoptotic potential. The compound 7b was found to significantly inhibit both cell lines and is therefore a promising therapeutic candidate for targeting both wild-type and mutant B-Raf forms.

show abstract

Section: Methodsmentioning

confidence: 99%

“…Measured the absorbance at OD570 nm for each well on an absorbance plate reader. [22] Morphological screening of compounds against A375 and Skmel-23 cells…”

Section: Mtt Assay Protocolmentioning

confidence: 99%

Discovery of Novel 1,2,4‐Oxadiazolyl Triazole Hybrids as B‐Raf Inhibitors for the Treatment of Melanoma

Pingili¹,

Svum²,

Raghavendra

2022

ChemistrySelect

View full text Add to dashboard Cite

show abstract

Synthesis, Antimicrobial Activity and Molecular Docking Studies of 1,3‐Thiazole Derivatives Incorporating Adamantanyl Moiety

Łączkowski

Misiura

Biernasiuk

et al. 2015

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

Synthesis, characterization and investigation of antimicrobial activity of 11 novel adamantanyl‐thiazoles are presented. Their structures were determined using 1H and 13C NMR, EI(+)‐MS, HRMS, and elemental analyses. Among the derivatives, compound 3c showed very strong activity, especially against Candida albicans ATCC 10231 and Candida parapsilosis ATCC 22019 with minimal inhibitory concentration (MIC) values ranging from 1.95 to 7.81 µg/ml. Compounds 3a and 3b showed good antifungal activity. Among the examined compounds, the widest spectrum of antibacterial activity possessed 3f that showed good activity, especially against Staphylococcus epidermidis ATCC 12228, Micrococcus luteus ATCC 10240, Bacillus subtilis ATCC 6633 with MIC values ranging from 31.25 to 62.5 µg/ml. Molecular docking studies of all compounds on the active sites of microbial enzymes indicated possible targets sterol 14α‐demethylase, secreted aspartic proteinase (SAP), N‐myristoyltransferase (NMT), and topoisomerase II. Thiazoles 3a, 3b, 3c, 3d, 3e, 3f, 3g, 3h, 3i, 3j, 3k showed more favorable affinity to SAP and NMT than the native ligand.

show abstract

Theoretical calculation of NMR shifts in newly developed antibacterial 4-formylbenzoic acid-based thiazoles

Baranowska-Łączkowska

Kozak

Łączkowski

et al. 2018

Theor Chem Acc

View full text Add to dashboard Cite

Thiazole Containing Nitrogen Mustards: Synthesis, Structural Evaluation, Cytotoxicity and DNA Binding Studies

Cited by 5 publications

References 39 publications

Discovery of Novel 1,2,4‐Oxadiazolyl Triazole Hybrids as B‐Raf Inhibitors for the Treatment of Melanoma

Discovery of Novel 1,2,4‐Oxadiazolyl Triazole Hybrids as B‐Raf Inhibitors for the Treatment of Melanoma

Synthesis, Antimicrobial Activity and Molecular Docking Studies of 1,3‐Thiazole Derivatives Incorporating Adamantanyl Moiety

Theoretical calculation of NMR shifts in newly developed antibacterial 4-formylbenzoic acid-based thiazoles

Contact Info

Product

Resources

About