65490-08-6

Upstream product

• 89-84-9 2',4'-dihydroxy-4-acetophenone 
• 107-30-2 chloromethyl methyl ether 
• 67-56-1 methanol 
• 130483-43-1 1-<2-hydroxy-4-(methoxymethoxy)phenyl>-3-phenylpropane-1,3-dione 
• 13057-17-5 bromethyl methyl ether 
• 109-87-5 Dimethoxymethane 
• 108-46-3 recorcinol 

Downstream Products

• 109723-83-3 2'-hydroxy-4'-methoxymethoxy-3,4-methylenedioxy-trans-chalcone 
• 111797-31-0 (E)-1-(2-hydroxy-4-(methoxymethoxy)phenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one 
• 126686-32-6 (E)-1-(2-hydroxy-4-(methoxymethoxy)phenyl)-3-phenylprop-2-en-1-one 
• 109471-14-9 (2E)-1-[2-hydroxy-4-(methoxymethoxy)phenyl]-3-(4-methoxyphenyl)prop-2-en-1-one 
• 110048-21-0 2'-hydroxy-3,4-dimethoxy-4'-methoxymethoxy-trans-chalcone 
• 110048-98-1 2'-hydroxy-2,3-dimethoxy-4'-methoxymethoxy-trans-chalcone 
• 124775-22-0 1-<2-Hydroxy-4-(methoxymethoxy)phenyl>-3-<4-(methoxymethoxy)phenyl>prop-2-en-1-on 
• 119100-24-2 2'-Hydroxy-3-methoxy-4,4'-bis(methoxymethoxy)chalcone 
• 141330-17-8 3-<2,4-Bis(methoxymethoxy)phenyl>-1-<2-hydroxy-4-(methoxymethoxy)phenyl>prop-2-en-1-on 
• 111492-45-6 3-(5-methoxymethoxy-2,2-dimethyl-2H-benzopyran-6-yl)-1-(2-hydroxy-4-methoxymethoxyphenyl)prop-2-en-1-one 
• 91078-12-5 (E)-1-(2-Hydroxy-4-methoxymethoxy-phenyl)-3-(5-methoxymethoxy-2,2-dimethyl-3-phenylsulfanyl-chroman-6-yl)-propenone 
• 91078-12-5 3-(5-methoxymethoxy-2,2-dimethyl-3-phenylthiochroman-6-yl-)-1-(2-hydroxy-4-methoxymethoxyphenyl)prop-2-en-1-one 
• 164031-43-0 3-(4-bromophenyl)-1-<2-hydroxy-4-(methoxymethoxy)phenyl>propane-1,3-dione 
• 130483-43-1 1-<2-hydroxy-4-(methoxymethoxy)phenyl>-3-phenylpropane-1,3-dione 

Relevant academic research and scientific papers

New Seco-DSP derivatives as potent chemosensitizers

Thirty-four seco-3′R,4′R-disubstituted-2′,2′-dimethyldihydropyrano[2,3-f]chromone (seco-DSP) derivatives were designed, synthesized and evaluated for chemo-reversal activity when combined with paclitaxel or vincristine in P-gp overexpressing A2780/T and KB-VIN drug-resistant cancer cell lines. Most of the compounds displayed moderate to significant MDR reversal activities. Compound 7e showed the most potent chemo-sensitization activity with more than 1471 reversal ratio at a concentration of 10 μM, which was higher than verapamil (VRP) (212-fold). Unexpectedly the newly synthesized compounds did not show chemosensitization activities in a non-P-gp overexpressing cisplatin resistant human ovarian cancer cell line (A2780/CDDP), implying that the MDR reversal effects might be associated with P-gp overexpression. Moreover, the compounds did not exhibit significant anti-proliferative activities against non-tumorigenic cell lines (HUVEC, HOSEC and T29) compared to VRP at the tested concentration and might be safer than VRP. In preliminary pharmacological mechanism studies, the compounds increased accumulation of DOX and promoted P-gp ATPase activity in A2780/T cell lines. Western blot analysis indicated they did not affect the expression level of P-gp in the tested MDR cell lines. Thus, further studies on these seco-DSP derivatives are merited with the goal of developing a desirable chemosensitizer drug candidate.

Design, synthesis and biological evaluation of millepachine derivatives as a new class of tubulin polymerization inhibitors

A series of novel tubulin polymerization inhibitors (9a-9p) have been synthesized and evaluated for their in vitro and in vivo biological activities. Among these compounds, 9e displayed strong antiproliferative activity against several tumor cell lines (I

Total Synthesis of the Natural Chalcone Lophirone E, Synthetic Studies toward Benzofuran and Indole-Based Analogues, and Investigation of Anti-Leishmanial Activity

The potential of natural and synthetic chalcones as therapeutic leads against different pathological conditions has been investigated for several years, and this class of compounds emerged as a privileged chemotype due to its interesting anti-inflammatory

Flavonoid-triazolyl hybrids as potential anti-hepatitis C virus agents: Synthesis and biological evaluation

A series of flavonoid-triazolyl hybrids were synthesized and evaluated as novel inhibitors of hepatitis C virus (HCV). The results of anti-HCV activity assays showed that most of the synthesized derivatives at a concentration of 100 μg/mL inhibited the ge

KRAS G12D INHIBITORS

The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

Flavonoid glycosides with a triazole moiety for marine antifouling applications: Synthesis and biological activity evaluation

Over the last decades, antifouling coatings containing biocidal compounds as active ingre-dients were used to prevent biofouling, and eco-friendly alternatives are needed. Previous research from our group showed that polymethoxylated chalcones and glycosy

Exploring the 2′-hydroxy-chalcone framework for the development of dual antioxidant and soybean lipoxygenase inhibitory agents

2′-hydroxy-chalcones are naturally occurring compounds with a wide array of bioactiv-ity. In an effort to delineate the structural features that favor antioxidant and lipoxygenase (LOX) inhibitory activity, the design, synthesis, and bioactivity profile of a series of 2′-hydroxy-chalcones bearing diverse substituents on rings A and B, are presented. Among all the synthesized derivatives, chalcone 4b, bearing two hydroxyl substituents on ring B, was found to possess the best combined activity (82.4% DPPH radical scavenging ability, 82.3% inhibition of lipid peroxidation, and satisfac-tory LOX inhibition value (IC50 = 70 μM). Chalcone 3c, possessing a methoxymethylene substituent on ring A, and three methoxy groups on ring B, exhibited the most promising LOX inhibitory activity (IC50 = 45 μM). A combination of in silico techniques were utilized in an effort to explore the crucial binding characteristics of the most active compound 3c and its analogue 3b, to LOX. A common H-bond interaction pattern, orienting the hydroxyl and carbonyl groups of the aromatic ring A towards Asp768 and Asn128, respectively, was observed. Regarding the analogue 3c, the bulky (-OMOM) group does not seem to participate in a direct binding, but it induces an orientation capable to form H-bonds between the methoxy groups of the aromatic ring B with Trp130 and Gly247.

Design, Synthesis, and Biological Evaluation of Icaritin Derivatives as Novel Putative DEPTOR Inhibitors for Multiple Myeloma Treatment

Icaritin is an active ingredient in Epimedium, which has a variety of pharmacological activities. However, the low activity of Icaritin and the unclear target greatly limit its application. Therefore, based on the structure of Icaritin, we adopted the str

Flavanone compound as well as preparation method and application thereof

The invention belongs to the technical field of medicines, and particularly relates to a flavanone compound as well as a preparation method and application thereof. Specifically disclosed is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The compound shown in the formula (I) can target hURAT1 and/or GLUT9, so that uric acid excretion is promoted, and the effect of reducing uric acid is achieved. The compound can be used for preparing medicines for treating and/or preventing and/or delaying and/or adjunctively treating and/or treating diseases related to hURAT1/GLUT9 activity, and has a good application prospect in preventing or treating diseases (such as gout, gouty arthritis, uric acid kidney stone and the like) related to hyperuricemia.

Synthesis and evaluation of butein derivatives for in vitro and in vivo inflammatory response suppression in lymphedema

Herein, we demonstrate that butein (1) can prevent swelling in a murine lymphedema model by suppressing tumor necrosis factor α (TNF-α) production. Butein derivatives were synthesized and evaluated to identify compounds with in vitro anti-inflammatory activity. Among them, 20 μM of compounds 7j, 7m, and 14a showed 50percent suppression of TNF-α production in mouse peritoneal macrophages after lipopolysaccharide stimulation. Compound 14a, exhibited the strongest potency with an in vitro IC50 of 14.6 μM and suppressed limb volume by 70percent in a murine lymphedema model. The prodrug strategy enabled a six-fold increase in kinetic solubility of compound 1 and five-fold higher levels of active metabolite in the blood for compound 14a via oral administration in the pharmacokinetics study. We suggest that the compound 14a could be developed as a potential therapeutic agent targeting anti-inflammatory activity to alleviate lymphedema progression.