1190630-27-3

Upstream product

• 149777-72-0 4-Bromo-2-methoxy-1-<(tert-butyldimethylsilyl)oxy>benzene 
• 1491173-73-9 1-(4-((tert-butyldimethylsilyl)oxy)-3-methoxyphenyl)prop-2-en-1-ol 
• 1094854-03-1 (S)-1-(3,4-dimethoxyphenyl)-1-oxopropan-2-yl-4-methylbenzenesulfonate 
• 1190630-26-2 C₁₈H₂₀O₅ 

Downstream Products

• 1190630-28-4 C₄₀H₄₈O₁₁ 

Relevant academic research and scientific papers

Evaluation of Manassantin A Tetrahydrofuran Core Region Analogues and Cooperative Therapeutic Effects with EGFR Inhibition

Tumors adapt to hypoxia by regulating angiogenesis, metastatic potential, and metabolism. These adaptations mediated by hypoxia-inducible factor 1 (HIF-1) make tumors more aggressive and resistant to chemotherapy and radiation. Therefore, HIF-1 is a validated therapeutic target for cancer. In order to develop new HIF-1 inhibitors for cancer chemotherapy by harnessing the potential of the natural product manassantin A, we synthesized and evaluated manassantin A analogues with modifications in the tetrahydrofuran core region of manassantin A. Our structure-activity relationship study indicated that the α,α′-trans-configuration of the central ring of manassantin A is critical to HIF-1 inhibition. We also demonstrated that a combination of manassantin A with an epidermal growth factor receptor inhibitor shows cooperative antitumor activity (～80% inhibition for combination vs ～30% inhibition for monotherapy). Our findings will provide important frameworks for the future therapeutic development of manassantin A-derived chemotherapeutic agents.

MANASSANTIN COMPOUNDS AND METHODS OF MAKING AND USING SAME

Provided are manassantin compounds and methods of using the compounds. Provided are methods of treating a disease, the method comprising administering a compound according to Formula I. Further provided are pharmaceutical compositions comprising compounds