1.Faculty of Pharmaceutical Sciences,Maharshi Dayanand University,Rohtak,India;2.Faculty of Pharmacy,Universiti Teknologi MARA (UiTM),Bandar Puncak Alam,Malaysia;3.Collaborative Drug Discovery Research (CDDR) Group, Pharmaceutical Life Sciences Community of Research,Universiti Teknologi MARA (UiTM),Shah Alam,Malaysia;4.Department of Pharmacology and Toxicology, College of Pharmacy,Qassim University,Buraidah,Kingdom of Saudi Arabia;5.Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns),Universiti Teknologi MARA (UiTM),Bandar Puncak Alam,Malaysia
Abstract:
Background
In view of wide range of biological activities of oxazole, a new series of oxazole analogues was synthesized and its chemical structures were confirmed by spectral data (Proton/Carbon-NMR, IR, MS etc.). The synthesized oxazole derivatives were screened for their antimicrobial and antiproliferative activities.
Results and discussion
The antimicrobial activity was performed against selected fungal and bacterial strains using tube dilution method. The antiproliferative potential was evaluated against human colorectal carcinoma (HCT116) and oestrogen- positive human breast carcinoma (MCF7) cancer cell lines using Sulforhodamine B assay and, results were compared to standard drugs, 5-fluorouracil and tamoxifen, respectively.
Conclusion
The performed antimicrobial activity indicated that compounds 3, 5, 6, 8 and 14 showed promising activity against selected microbial species. Antiproliferative screening found compound 14 to be the most potent compound against HCT116 (IC50?=?71.8 µM), whereas Compound 6 was the most potent against MCF7 (IC50?=?74.1 µM). Further, the molecular docking study has been carried to find out the interaction between active oxazole compounds with CDK8 (HCT116) and ER-α (MCF7) proteins indicated that compound 14 and 6 showed good dock score with better potency within the ATP binding pocket and may be used as a lead for rational drug designing of the anticancer molecule.
