Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents

Jing-Ping Liou¹, Chun-Wei Chang, Jeng-Shin Song

¹Medicinal Synthetic Laboratory, Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 128 Yen-Chiu-Yuan Road, Sec II, Taipei 115, Taiwan, Republic of China.

|May 31, 2002

Abstract:

A new type of inhibitor of tubulin polymerization was discovered on the basis of the combretastatin molecular skeleton. The lead compounds in this series, compounds 6 and 7, strongly inhibited tubulin polymerization in vitro and significantly arrested cells at the G(2)/M phase. Compounds 6 and 7 yielded 50- to 100-fold lower IC(50) values than did combretastatin A-4 against Colo 205, NUGC3, and HA22T human cancer cell lines as well as similar or greater growth inhibitory activities than did combretastain A-4 against DLD-1, HR, MCF-7, DU145, HONE-1, and MES-SA/DX5 human cancer cell lines. Structure-activity relationship information revealed that introduction of an amino group at the ortho position of the benzophenone ring plays an integral role for increased growth inhibition.

Related Experiment Videos

Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents

Related Concept Videos

Stereoselectivity of Galactosylation Reactions In Vacuo.

Isorhoifolin regulates S1PR3-CK2-GSK3β axis and promotes neurite regrowth and functional recovery after traumatic brain injury.

Enhancing health and occupational performance: A group-based exercise programme for people with visual impairment.

Electrochemically Induced Structural Evolution to Generate Optimized High-Entropy-Alloy Electrocatalysts for Ethanol Oxidation.

Template-Confined Synthesis of 1 nm High-Entropy-Alloy Nanoparticle Library for Electrocatalysis.

Asymmetric Total Synthesis of C2-OH Lycopodium Alkaloids (-)-Palhinine B, (-)-Palhinine C, and (+)-Palhinine B Enabled by Stereocontrolled Diels-Alder Strategy.

Synthetic Heparan Sulfate-like Oligosaccharides as Tools to Decipher Growth Factor Recognition.

A Novel Trigonal Prismatic Rhenium Complex of 2-Hydroxythiobenzhydrazide as a Potent and Selective Anticancer Agent.

Bifunctional Ionophores for Cuproptosis Activation: Dual Targeting of Copper and Fe-S Protein Homeostasis.

Lead Optimization of Quinoline-Coumarin KRAS mRNA G-Quadruplex Ligands: Discovery of Non-Quaternary Ammonium Analogs as Translation Inhibitors.

Accurate Identification of Covalently Ligandable Cysteines Using CCSite.

High-Resolution Relaxometry for Fragment Screening.

Design, Synthesis, and Biological Evaluation of Anthracene Derivatives as Potent Antioxidants: Experimental, DFT, and Docking Studies.

Integrated in vitro and in silico evaluations of novel benzanilide derivatives as anticancer agents.

Total Synthesis-Assisted Structure Determination and Biological Evaluation of Cytotoxic Cyclodepsipeptide Destruxin F.

Discovery of Emodin as a novel competitive KPC-2 inhibitor through virtual screening: Synergistic efficacy with Meropenem against Carbapenem-resistant Klebsiella pneumoniae infection.

Design, Synthesis, Antimicrobial Evaluation, DFT Analysis, Molecular Docking and Molecular Dynamics Studies of Thiadiazol-Hydrazine Derivatives as Potential Dihydrofolate Reductase Inhibitors.

Syzygium aromaticum Attenuates Cerebellar Oxidative Stress: An Integrated in silico, in vitro, and in vivo Evaluation of Multi-Target Antioxidant Mechanisms.

Related Experiment Videos

Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents

Abstract:

Related Concept Videos

Related Articles