cox-2-in-1

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

EGFR COX-2-IN-1 is an EGFR COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR COX-2-IN-1 significantly increases the proportion of cells in the G2 M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.

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-1-IN-2 (compound 5h) serves as a potent anti-inflammatory and analgesic agent. This compound demonstrates a significant inhibitory effect on COX-1, with an IC 50 value of 38.76 nM.

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

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 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 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-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-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-1 2-IN-6 (compound 4 h) acts as a dual inhibitor of COX-1 and COX-2, exhibiting potent inhibitory activity with IC50 values of 68 nM and 91 nM, respectively. It is utilized in the research of inflammatory diseases [1].

COX-1 2-IN-8 (compound 11f) is an orally active inhibitor of both COX-1 and COX-2, with IC50 values of 2.14 µM and 0.58 µM, respectively. Its anti-inflammatory activity surpasses that of celecoxib.

COX-1 2-IN-9 (Compound 3n) serves as a selective and potent inhibitor of both COX-1 and COX-2, demonstrating IC 50 values of 0.031 µM for COX-1 and 0.01 µM for COX-2. This compound exhibits antibacterial and anti-inflammatory properties, effectively targeting MRSA 1478 (MIC=50 μg mL) and multidrug-resistant S. lentus (MIC=50 μg mL). Furthermore, COX-1 2-IN-9 shows promise in relieving MRSA-induced pneumonia in conditions of compromised immunity.