An article Design and Synthesis of Novel Nordihydroguaiaretic Acid (NDGA) Analogues as Potential FGFR1 Kinase Inhibitors With Anti-Gastric Activity and Chemosensitizing Effect WOS:000576019000001 published article about GASTRIC-CANCER; GENE AMPLIFICATION; BREAST-CANCER; PHASE-I; GROWTH; DISCOVERY; TERAMEPROCOL; CHALLENGES; AGENTS in [Chen, Qian; Li, Wulan] Wenzhou Med Univ, Affiliated Hosp 1, Wenzhou, Peoples R China; [Chen, Qian; Zhu, Min; Xie, Jingwen; Dong, Zhaojun; Khushafah, Fatehi; Yun, Di; Fu, Weitao; Wei, Tao; Liu, Zhiguo; Qiu, Peihong; Wu, Jianzhang; Li, Wulan] Wenzhou Med Univ, Coll Pharmaceut Sci, Chem Biol Res Ctr, Wenzhou, Peoples R China; [Wang, Ledan] Wenzhou Med Univ, Affiliated Hosp 2, Dept Gynecol & Obstet, Wenzhou, Peoples R China in 2020.0, Cited 49.0. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4. Application In Synthesis of 3-Hydroxybenzaldehyde
Aberrant fibroblast growth factor receptor-1 (FGFR1), a key driver promoting gastric cancer (GC) progression and chemo-resistance, has been increasingly recognized as a potential therapeutic target in GC. Hereon, we designed and synthesized a series of asymmetric analogues usingAf23and NDGA as lead compounds by retaining the basic structural framework (bisaryl-1,4-dien-3-one) and the unilateral active functional groups (3,4-dihydroxyl). Thereinto,Y14showed considerable inhibitory activity against FGFR1. Next, pharmacological experiments showed thatY14could significantly inhibit the phosphorylation of FGFR1 and its downstream kinase AKT and ERK, thus inhibiting the growth, survival, and migration of gastric cancer cells. Furthermore, compared with 5-FU treatment alone, the combination ofY14and 5-FU significantly reduced the phosphorylation level of FGFR1, and enhanced the anti-cancer effect by inhibiting the viability and colony formation in two gastric cancer cell lines. These results confirmed thatY14exerted anti-gastric activity and chemosensitizing effect by inhibiting FGFR1 phosphorylation and its downstream signaling pathwayin vitro. This work also provides evidence thatY14, an effective FGFR1 inhibitor, could be used alone or in combination with chemotherapy to treat gastric cancer in the future.
About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Chen, Q; Zhu, M; Xie, JW; Dong, ZJ; Khushafah, F; Yun, D; Fu, WT; Wang, LD; Wei, T; Liu, ZG; Qiu, PH; Wu, JZ; Li, WL or concate me.. Application In Synthesis of 3-Hydroxybenzaldehyde
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles