Cancer is a major death‐causing disease all over the world for the past few decades. A novel series of 1,2,3‐triazole tethered indole (7a‐l) derivatives have been synthesized and their structures were confirmed by 1HNMR, 13CNMR, and mass spectral data. All these compounds (7a –l) were screened for anticancer activity against two human cancer cell lines such as MCF‐7 and HepG‐2 cells by MTT assay. Compounds substituted with 4‐hydroxy, 4‐methoxy, 2‐methyl, and 3‐acetyl groups exhibited more potent activity against MCF‐7 and HepG‐2 cell lines with best IC50 values than standard reference Doxorubicin. Molecular docking studies performed on crystal structures of Aurora kinase‐1 and DNA topoisomerase‐2 alpha showed remarkable binding affinity values and key interactions as compared to the standard reference Doxorubicin.
A novel series of thiazole-triazole-piperazine multi hybrids was designed for antimicrobial activity
and the synthetic method for this series has been developed by copper catalyzed 1,3-dipolar
cycloaddition of thiazole-based azide with Boc-piperidine based alkyne in the presence of CuSO4 and
sodium ascorbate. Boc deprotection followed by alkylation of piperidine moiety in hybrid derivatives
was also carried out. All the target compounds were confirmed using FTIR, 1H NMR, 13C NMR and
LC-MS spectral techniques. These compounds were screened for the antimicrobial activity against
bacteria and fungi. The antimicrobial activities are also comparable to standard drugs ampicillin and
clotrimazole. All the molecules showed good to moderate activity and supported by molecular docking
studies and ADME prediction.
PCD obviates surgery or acts as a temporizing measure in a significant number of patients with necrotizing pancreatitis. APACHE II scores and extent of intrapancreatic necrosis are principle factors determining success of PCD.
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