Structural optimization of indole based compounds for highly promising anti-cancer activities: structure activity
1UGC Sponsored Centre for Advanced Studies, Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
Abstract:
Based on the anti-cancer data of previous compounds, 27 more compounds were synthesized and subjected to anti-cancer screening. Compounds were tested over 60 human tumor cell lines of different types of cancer. As per the data available, some compounds exhibited appreciable anti-cancer properties over certain cell lines with their GI₅₀ in nM range. With the help of UV-vis spectral studies, enzyme immunoassay and molecular modeling studies, dihydrofolate reductase was found to be the probable cellular target of the compounds under present investigation.
More Related Videos
Related Concept Videos
Drug Discovery: Overview
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
The direct-acting...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Local Anesthetics: Chemistry and Structure-Activity Relationship


