Synthesis and biological activity
Medicinal chemists working on synthesis and biological activity design small organic molecules—often built around ring-containing frameworks called heterocycles—and then test how those structures interact with specific biological targets linked to disease. Compounds such as chalcones, coumarins, and pyrazoles have drawn sustained attention because subtle changes to their ring systems or substituents can dramatically shift potency, selectivity, and toxicity profiles, particularly against cancer cells where disrupting proteins like tubulin can halt tumor growth or collapse the blood vessels that feed it. A central challenge is translating promising in-vitro activity into drug candidates that remain effective and safe in living systems, which requires understanding not just what a compound does but why its three-dimensional shape enables it to do so. Ongoing work is pushing toward rational, structure-guided design and the exploration of hybrid molecules that combine two pharmacophores in a single scaffold, aiming to overcome the resistance mechanisms that limit existing anticancer therapies.
- Works
- 99,462
- Total citations
- 930,629
- Keywords
- Heterocyclic CompoundsMedicinal ChemistryAnticancer AgentsTubulin InhibitorsVascular Targeting AgentsChalcones
Top papers in Synthesis and biological activity
Ordered by total citation count.
- Mitogen-Activated Protein Kinase Pathways Mediated by ERK, JNK, and p38 Protein Kinases↗ 4,307
- Multicomponent Reactions with Isocyanides↗ 4,045
- A Knowledge-Based Approach in Designing Combinatorial or Medicinal Chemistry Libraries for Drug Discovery. 1. A Qualitative and Quantitative Characterization of Known Drug Databases↗ 3,063
- Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase↗ 3,037OA
- Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer↗ 2,802
- The Properties of Known Drugs. 1. Molecular Frameworks↗ 2,516
- Molecular Docking and Structure-Based Drug Design Strategies↗ 2,502OA
- Chemistry of Heterocyclic Compounds↗ 2,450
- Isolation, Structure, and Partial Synthesis of an Active Constituent of Hashish↗ 2,383
- Molecular Docking: Shifting Paradigms in Drug Discovery↗ 2,296OA
- Flavonoids: antioxidants or signalling molecules?↗ 2,009
- Synthesis and Biological Evaluation of the 1,5-Diarylpyrazole Class of Cyclooxygenase-2 Inhibitors: Identification of 4-[5-(4-Methylphenyl)-3- (trifluoromethyl)-1<i>H</i>-pyrazol-1-yl]benzenesulfonamide (SC-58635, Celecoxib)↗ 1,965OA
Active researchers
Top authors in this area, ranked by h-index.