Li, Xinyu published the artcileSynthesis and biological evaluation of 3-aryl-quinoline derivatives as anti-breast cancer agents targeting ERα and VEGFR-2, Related Products of isoquinoline, the main research area is antitumor arylquinoline estrogen receptor alpha VEGFR 2 multi target; arylquinoline SAR anti breast cancer multi target; Anti-breast cancer; Estrogen receptor; Multi target; VEGFR-2.
Selective estrogen receptor modulators(SERMs) are a series of important small mol. compounds to modulate the estrogen receptor, such as tamoxifen. Although these drugs have shown great benefits in the treatment of breast cancer, the risk of endometrial cancer and endocrine resistance restrict their use. The reasonable designing of multi-target drugs can decrease the side effects and improve the tolerance of antineoplastic agents. Studies have identified that VEGFR-2 plays a pivotal role in tumor angiogenesis and drug resistance. Besides, a combination of Tamoxifen and a low dose of a VEGFR-2 inhibitor was reported to maximize therapeutic efficacy as well as to retard SERM resistant tumor growth. In this work, a series of 3-aryl-quinoline derivatives were designed to target ERα and VEGFR-2 to eliminate the disadvantages of SERMs. We identified that compounds I [R1 = H, R2 = MeO; R1 = MeO, R2 = H] displayed highly ER binding affinities as well as relative intensity VEGFR-2 inhibitory activities. Moreover, these two compounds exhibited excellent anti-proliferative activities against MCF-7 and HUVEC cell lines with low micromolar IC50 (1-8 μM). A further study confirmed that compound I [R1 = MeO, R2 = H] can reduce the expression of PgR mRNA, arrest cell cycle in MCF-7 breast cancer cells, and restrain the cell migration. Overall, based on the biol. activities data, I [R1 = MeO, R2 = H] can be chosen as a potential anti-cancer lead compound for further studying.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Related Products of isoquinoline.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem