cox-2

COX-2-IN-34 is a selective, orally potent COX-2 inhibitor that shows anti-inflammatory activity without gastric ulcer toxicity during experiments in mice.

COX-2-IN-2, a selective inducible COX2 inhibitor, exhibits potent inhibition with an IC50 of 0.24 μM. Meanwhile, COX-2-IN-1 functions as an anti-inflammatory agent, demonstrating both anti-inflammatory and analgesic activities.

COX-2-IN-1 is a potent and selective COX-2 inhibitor (IC50: 3.9 μM).

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

COX-2-IN-31 (compound 7b) is an orally active dual inhibitor targeting COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM), and also inhibits transmembrane hCA IX (Ki=48.9 nM) and hCA XII (Ki=5.8 nM), demonstrating anti-inflammatory and analgesic activity [1].

COX-2-IN-32 (Compound 2f) is a dual inhibitor of iNOS and COX-2 that downregulates NF-κB expression and demonstrates anti-inflammatory properties by impeding NO production in LPS-induced RAW264.7 macrophages with an IC50 value of 11.2 μM [1].

COX-1 2-IN-4 (compound 2b) is a dual COX-1 and COX-2 inhibitor with IC50 values of 0.239 μM for COX-1 and 0.191 μM for COX-2, and demonstrates moderate anticancer activity with IC50 values of 30.79 μM against COLO205 cancer cell lines and 74.15 μM against B16F1 cancer cell lines [1].

COX-2 NO-IN-1 is an orally active nitric oxide synthase (iNOS) and NO (IC50 of 3.52 μM) inhibitor that also suppresses COX-2 expression, exhibiting anti-inflammatory effects and reducing pathological damage to kidney tissues [1].

COX-2-IN-7 (compound 4a) is a potent and selective COX-2 inhibitor with greater selectivity than Celecoxib and an IC50 value of 6.585 µM. It exhibits good anti-inflammatory properties and low ulcerogenic activity in vivo[1].

COX-2-IN-18 (Compound 3) is a highly effective COX-2 inhibitor with an IC50 value of 0.775 μM, demonstrating strong inhibitory activity against COX-2. Its potency is comparable to the reference drug Celecoxib (IC50 = 0.153 μM), showing promise in the field of cancer research [1].

COX-2-IN-11 (compound 7b2) is a potent and selective COX-2 inhibitor with potential applications in inflammation disease research[1].

COX-2-IN-22 is a COX-2 inhibitor (IC50: 8.6 μM) that can cross the blood-brain barrier and also exhibits inhibitory effects on AChE (IC50: 2.8 μM), BChE (IC50: 6.3 μM), β-Secretase (IC50: 15.3 μM), LOX-5 (IC50: 13.9 μM) and DPPH ( IC50: 6.8 μM) showed inhibitory effects.

COX-2-IN-35 (compound 7) is a selective COX-2 inhibitor with anti-inflammatory activity, exhibiting an inhibitory concentration (IC 50) of 4.37 nM [1].

COX-2 15-LOX-IN-1 (Compound 14) is a dual inhibitor of COX-2 and 15-lipoxygenase (15-LOX) with IC50 values of 10.65 μM for COX-1, 0.075 μM for COX-2, and 2.98 μM for 15-LOX, exhibiting an anti-inflammatory effect.

COX-2-IN-16 (compound 2b) is a potent, selective, and orally active inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 102 μM, effectively reducing nitric oxide (NO) production and demonstrating anti-inflammatory activity [1].

COX-2-IN-8 (Compound 6a) is a potent, selective, orally active COX-2 inhibitor (IC50: 6.585 μM) with a higher COX-2 selectivity than Celecoxib.

COX-2-IN-19 (Compound 24) is a highly potent cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1.76 μM, exhibiting significant in vivo anti-inflammatory activity [1].

COX-2-IN-23 is a selective inhibitor of COX-2, with IC50 values of 0.28 and 20.14 μM for COX-2 and COX-1, respectively.COX-2-IN-23 exhibits anti-inflammatory effects as well as low ulcerogenic effects.

COX-2-IN-13 (compound 13e) is a highly potent and selective COX-2 inhibitor with an impressive IC50 value of 0.98 μM. It exhibits strong anti-inflammatory activity and has shown favorable results in in vivo acute toxicity studies [1].

COX-2-IN-10 is a potent COX-2 inhibitor that exhibits inhibitory effects on the production of IL-6, TNF-α, and IL-1β, and inhibits PGE2 production in a concentration-dependent manner with an IC50 value of 2.54 μM. Additionally, COX-2-IN-10 inhibits the expression of iNOS and COX-2 at both mRNA and protein levels.

COX-2-IN-14 (compound 2a) is a highly potent and selective inhibitor of COX-2 (cyclooxygenase-2), binding strongly at the active site of the COX-2 co-crystal. Demonstrating remarkable in vivo anti-inflammatory activity, COX-2-IN-14 effectively reduces ear edema and myeloperoxidase (MPO) activity in mice [1].

COX-2 PI3K-IN-2 (compound 5f) possesses anti-inflammatory and anti-cancer properties, functioning as a selective inhibitor of COX-2 (Ki = 3.02 nM) and a potent inhibitor of PI3K (IC50 = 2.78 nM) [1].

COX-2 15-LOX-IN-4 (compound 5i) is a dual inhibitor with IC50 values of 0.075 μM for COX-2 and 1.97 μM for 15-LOX. It inhibits LPS-induced production of pro-inflammatory cytokines (IL-6, ROS) and exhibits targeted anti-inflammatory effects [1].

COX-2-IN-28 is a potent and selective COX-2 inhibitor, with IC50 values of 0.054 μM for COX-2, 2.14 μM for 15-LOX, and 13.21 μM for COX-1.

Topo I COX-2-IN-2 (Compound W10) is a potent dual inhibitor of Topo I (IC50: 0.90 μM) and COX-2 (IC50: 2.31 μM), inducing apoptosis in cancer cells via the mitochondrial pathway.

COX-2/sEH-IN-1 is an orally active dual inhibitor of COX-2 (IC50: 1.24 μM) and sEH (IC50: 0.40 μM), a soluble epoxide hydrolase. COX-2/sEH-IN-1 increases anti-inflammatory effects and significantly reduces cardiovascular risk.

COX-2-IN-20 (Compound 5d) is a selective and orally active COX-2 inhibitor (IC50 = 17.9 nM) with anti-inflammatory activity [1].

COX-2-IN-12 (compound 3b) is a potent and selective COX-2 inhibitor with an IC50 of 19.98 μM, demonstrating anti-inflammatory properties and safety in in-vivo acute toxicity studies [1].

COX-2 5-LOX-IN-3 (compound 5b) is a powerful dual inhibitor of COX-2 and 5-LOX, with IC50 values of 45.73 μM, 5.45 μM, and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively, showing promise for the investigation of inflammatory diseases [1].

COX-2-IN-24 is an orally active COX-2 inhibitor [IC50: 0.17 μM] with anti-inflammatory and hypo-ulcerogenic effects.

COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].

COX-2 15-LOX-IN-2 is a potent inhibitor of COX-2 (IC50: 0.065 μM) and 15-LOX (IC50: 1.86 μM), also demonstrating significant antioxidant activity [1].

COX-2 5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent dual inhibitor of COX-2 and 5-LOX, exhibiting superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. It demonstrates strong inhibitory activity against COX-1, COX-2, and 5-LOX, with IC50 values of 12.13 μM, 0.4 μM, and 4.96 μM, respectively [1].

COX-2-IN-26 is a potent, orally active, selective COX-2 inhibitor, acting on COX-1 (IC50: 10.61 μM), COX-2 (IC50: 0.067 μM), and 15-LOX (IC50: 1.96 μM). COX-2-IN-26 is anti-inflammatory and possesses a gastrointestinal safety profile.

COX-2 PI3K-IN-1 (compound 5d) is a potent inhibitor of PI3K with an IC50 of 1.14 nM and selectively inhibits COX-2 with a Ki of 3.24 nM.

COX-2-IN-9 is a selective, potent, orally active COX-2 inhibitor (IC50: 10.17 μM).COX-2-IN-9 has a higher COX-2 selectivity than Celecoxib.COX-2-IN-9 exhibits good in vivo anti-inflammatory activity and low ulcerogenic effect.

COX-2-IN-33 (compound 5f) is a selective COX-2 inhibitor with an IC50 of 45.5 nM, demonstrating potential as an anti-inflammatory agent by effectively suppressing pro-inflammatory cytokine production in vivo while maintaining gastric safety [1].

COX-2 15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2 and 15-LOX with inhibitory concentrations (IC50) of 0.075 μM and 1.97 μM, respectively. This compound effectively suppresses LPS-induced production of pro-inflammatory cytokines (IL-6, ROS, and NO), exhibiting targeted anti-inflammatory effects [1].

COX-1 2-IN-5 (compound 2a) is a dual inhibitor of COX1 2, demonstrating inhibitory concentrations (IC50) of 2.650 μM and 0.958 μM, respectively, and exhibits anticancer activity against liver cancer HepG2 cells with an IC50 of 60.75 μM [1].

COX-2-IN-29 is a selective inhibitor of orally active COX-2 (IC50: 0.005 μM).

COX-2-IN-17 is a potent, blood-brain barrier permeable COX-2 (cyclooxygenase-2) inhibitor (IC50: 0.02 μM) with anti-inflammatory and analgesic activity.

COX-1 2-IN-3 (Compound 7a) is a dual inhibitor of COX-1 and COX-2, exhibiting anti-inflammatory activity with low toxicity [1].

COX-2 5-LOX-IN-2 is a benzothiophen-2-ylpyrazole carboxylic acid derivative that inhibits both COX-2 and 5-LOX. COX-2 5-LOX-IN-2 (5b) has IC50 values of 5.40, 0.01, and 1.78 μM for COX-1, COX-2, and 5-LOX, respectively, and exhibits greater analgesic and anti-inflammatory activities than Celecoxib and Indomethacin.

COX-1/2-IN-2, a potent inhibitor of both COX-1 and COX-2, demonstrates significant inhibitory activity, with IC50 values of 13.9 ± 3.21 μM for COX-1 and 6.4 ± 0.74 μM for COX-2, respectively [1].

COX-1 2-IN-2 is a potent inhibitor of both COX-1 and COX-2, with IC50 values of 9.7 ± 0.09 μM for COX-1 and 4.6 ± 1.45 μM for COX-2, respectively [1].

Topo I COX-2-IN-1 (1H-30) is a potent Topo I COX-2 inhibitor with IC50 values of 0.24 μM for COX-2 and 4.42 μM for Topo I. It induces apoptosis and inhibits cancer cell migration, demonstrating anti-cancer activity.

COX-2-IN-21 (Compound 5c) is an orally active, selective COX-2 inhibitor with an IC50 of 0.039 μM, demonstrating significant anti-inflammatory potential.