Ring‐B Modification of Combretastatin A‐4 to Generate Thiazolidine‐2,4‐dione‐1,2,3‐triazole Hybrids as Tubulin Polymerization Inhibitors

Vanaparthy, Advaitha; Bokkala, Karthik; Thirukovela, Narasimha Swamy; Sirassu, Narsimha; Manchal, Ravinder; Srinivas, Bandari; Nukala, Satheesh Kumar

doi:10.1002/slct.202301179

Cited by 3 publications

(1 citation statement)

References 54 publications

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“…In continuation of our work to synthesize biologically active hybrids, [24][25][26][27] here we have designed (Figure 2) the compounds that consists of two pharmacophores (quinoline and isoxazole) by taking in to consideration of the above stated biological applications of isoxazole and quinoline and advantages of the pharmacophore hybridization. [28,29] Results and Discussion Chemistry Synthesis of the target compounds (5 a-5 n) was achieved in three steps as shown in Scheme 1.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Fused Isoxazoles of Iodoquinol as in vitro EGFR Aiming Anticancer Agents

Bokkala,

Bapuram,

Thirukovela

et al. 2024

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We have presented the synthesis of some new quinoline linked fused isoxazoles via copper (I) catalyzed azide alkyne cycloaddition (CuAAC) followed by intramolecular C−H arylation of isoxazole ring using PdCl2(PPh3)2 catalyst. All the synthesized compounds were investigated for anticancer activity against three human breast cancer cell lines such as MCF‐7, MDA‐MB‐468 and MDA‐MB‐231 using MTT assay and 5‐fluorouracil (5‐FU) was used as a standard drug. In this study, three compounds were exhibited greater activity than reference drug 5‐FU against three cell lines which further screened for in vitro tyrosine kinase EGFR inhibition and molecular docking studies by taking EGFR protein as the target. Finally, insilico pharmacokinetic profile of the same compounds was obtained using SWISSADME where two compounds following Lipinski, Ghose, Veber, Egan, and Muegge rules.

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Section: Introductionmentioning

confidence: 99%

Synthesis of Fused Isoxazoles of Iodoquinol as in vitro EGFR Aiming Anticancer Agents

Bokkala,

Bapuram,

Thirukovela

et al. 2024

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Fused Imidazo[1,2‐d][1,2,4]Thiadiazolo[1,2,3]Triazoles: One‐Pot Synthesis, Anti‐Bacterial, Anti‐Biofilm and TLR4 Inhibitory Activities

Premalatha,

Azam,

Kapavarapu

et al. 2024

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We developed and evaluated several new fused imidazo[1,2‐d][1,2,4]thiadiazolo[1,2,3]triazoles to see how they perform against bacteria and biofilms. Some compounds showed acceptable activity compared to the primary standard, Dicloxacillin. Some of the compounds demonstrated significant antibacterial activity against S. aureus, with MIC values ranging from 1.56–12.5 μg/mL. We also found anti‐biofilm properties in the potent compounds. The results showed that derivatives 3‐(4‐fluorophenyl)imidazo[1,2‐d] [1,2,3] triazolo[1,5‐b][1,2,4]thiadiazole 8,8‐dioxide and 3‐(3,5‐difluorophenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b][1,2,4] thiadiazole 8,8‐dioxide were strong antibacterial agents and effective MSSA and MRSA biofilm growth inhibitors. We conducted in silico studies to assess the molecular interactions of more potent compounds with TLR4 proteins (PDB: 3FXI, 3VQ1, 3RG1). Our findings revealed that 3‐(4‐chloro‐3,5‐dimethoxyphenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b] [1,2,4]thiadiazole 8,8‐dioxide, 3‐(3,5‐dichlorophenyl)imidazo[1,2‐d] [1,2,3]triazolo[1,5‐b][1,2,4] thiadiazole 8,8‐dioxide, and 3‐(4‐(trifluoromethyl)phenyl)imidazo[1,2‐d][1,2,3]triazolo[1,5‐b][1,2,4] thiadiazole 8,8‐dioxide exhibited more binding interactions than dicloxacillin. ADME of more potent compounds examined in this study and compounds could potentially inhibit the cytochrome P450 CYP2C19 isoform.

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Synthesis of Some New Barbituric Acid Linked Quinoline-1,2,3-triazole Hybrids as Dual EGFR/VEGFR-2 Inhibitors

Mamidala,

Thirukovela,

Bapuram

et al. 2024

Russ J Gen Chem

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Ring‐B Modification of Combretastatin A‐4 to Generate Thiazolidine‐2,4‐dione‐1,2,3‐triazole Hybrids as Tubulin Polymerization Inhibitors

Cited by 3 publications

References 54 publications

Synthesis of Fused Isoxazoles of Iodoquinol as in vitro EGFR Aiming Anticancer Agents

Synthesis of Fused Isoxazoles of Iodoquinol as in vitro EGFR Aiming Anticancer Agents

Fused Imidazo[1,2‐d][1,2,4]Thiadiazolo[1,2,3]Triazoles: One‐Pot Synthesis, Anti‐Bacterial, Anti‐Biofilm and TLR4 Inhibitory Activities

Synthesis of Some New Barbituric Acid Linked Quinoline-1,2,3-triazole Hybrids as Dual EGFR/VEGFR-2 Inhibitors

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