Synthesis and biological activity
Medicinal chemists working at the intersection of organic synthesis and pharmacology design and build heterocyclic compounds—ring-shaped molecules containing atoms such as nitrogen, oxygen, or sulfur—to understand how small structural changes translate into measurable biological effects. Much of the current effort centers on molecules like chalcones, coumarins, and pyrazoles, which have shown promise as anticancer agents by disrupting tubulin polymerization or starving tumors of their blood supply through vascular targeting. Researchers are actively trying to understand why certain scaffolds bind selectively to disease-relevant proteins while sparing healthy tissue, and how synthetic modifications can sharpen that selectivity without sacrificing potency or introducing toxicity. Open questions include how to move the most promising candidates reliably from in vitro screens into animal models, and how to exploit the structural versatility of heterocycles to address cancers that have developed resistance to existing therapies.
- Works
- 98,880
- Total citations
- 921,271
- 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↗ 4,295
- Multicomponent Reactions with Isocyanides↗ 4,039
- Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase↗ 3,028OA
- A Knowledge-Based Approach in Designing Combinatorial or Medicinal Chemistry Libraries for Drug Discovery. 1. A Qualitative and Quantitative Characterization of Known Drug Databases↗ 3,026
- Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer↗ 2,795
- The Properties of Known Drugs. 1. Molecular Frameworks↗ 2,454
- Chemistry of Heterocyclic Compounds↗ 2,450
- Molecular Docking and Structure-Based Drug Design Strategies↗ 2,449OA
- Isolation, Structure, and Partial Synthesis of an Active Constituent of Hashish↗ 2,375
- Molecular Docking: Shifting Paradigms in Drug Discovery↗ 2,233OA
- Flavonoids: antioxidants or signalling molecules?↗ 2,005
- 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)↗ 1,956OA
Active researchers
Top authors in this area, ranked by h-index.