antitumor agent

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

Antitumor agent-19 is a modulator of tumor-associated macrophages with EC50s of 17.18 μM and 18.87 μM in the RAW 264.7 cells and the BMDM cells.

Antitumor agent-4 is a butenylphenyl phosphate derivative, is an agent of mammary cancer and anovulatory sterility.

Antitumor agent-3, a potent compound, comprises a novel imidazopyridine with excellent antitumor activity as its active ingredient.

Antitumor agent-185 (compound 3) exhibits significant antitumor effects, effectively inhibiting tumor growth and extending the survival period of mice in vivo.

Antitumor Agent-184 (compound 12aa) triggers apoptosis in various cell lines, exhibiting IC50 values of 2.35 μM in B16-F10 cells, 7.32 μM in 4T1 cells, and 10.31 μM in CT26 cells.

Antitumor agent-188 (compound C6) exhibits α-glucosidase inhibitory activity and anticancer properties. It induces excessive ROS production, thereby triggering oxidative stress.

Antitumor agent-189 (Compound DN4) is an effective anticancer drug. It inhibits the proliferation, adhesion, and invasion of A498 cells, with an IC50 of 1.94 μM. Additionally, Antitumor agent-189 suppresses angiogenesis and tumor growth in heterotopic xenograft models of A498 cells.

Antitumor agent-187 (compound I) is an isoflavone derivative with antitumor activity. It exhibits IC50 values of 5.23 μM and 2.63 μM against A2780 and SKOV3 cell lines, respectively.

Antitumor agent-160 (compound Ia) is a derivative of the antifungal agent PHENALENONE and exhibits antitumor activity.

Antitumor agent-192 (Compound 2f) is a β-carboline antitumor compound. It induces autophagy in HCT116 cells via the ATG5/ATG7 pathway. The IC50 of Antitumor agent-192 against human tumor cell lines is below 5 μM, and it significantly inhibits tumor growth and reduces tumor weight in xenograft mouse models of colorectal cancer.

Antitumor agent-191 (Compound 7) exhibits antiviral activity against HSV-1 and HIV, with EC50 values of 0.03 μM and 0.81 μM, respectively. It also demonstrates potential antitumor properties by inhibiting cancer cell lines HepG2, WI-38, Vero, and MCF-7, with IC50 values of 19.6, 39.3, 18.3, and 28 μM, respectively.

Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer properties, exhibiting an IC50 of 90 nM against MCF-7 breast cancer cells. This compound induces apoptosis by modulating the Bax-caspase 3 signaling pathway and triggers ferroptosis by regulating key signaling molecules (including GPX4). Antitumor agent-196 shows potential for cancer research applications.

Antitumor agent-195 (compound 16c) is a dual-targeting agent that simultaneously targets STAT3 and NQO1. At a concentration of 1 μM, it significantly inhibits the phosphorylation of STAT3 at the Tyr705 site and effectively induces apoptosis in MDA-MB-231 and MDA-MB-468 breast cancer cells. As a substrate of NQO1, Antitumor agent-195 markedly increases ROS production, causing severe DNA damage in a dose-dependent manner. It also demonstrates strong antitumor properties in MDA-MB-231 xenograft models.

Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, effectively inhibiting the proliferation of CAL27, HN6, HN30, SCC9, and SCC25, with an IC50 ranging from 4 nM to 77 nM. Additionally, Antitumor agent-198 suppresses HNSCC cell migration, arrests the cell cycle, and induces apoptosis.

Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor that binds to the colchicine site on tubulin, causing G2/M cell cycle arrest and inducing reactive oxygen species (ROS) production. It demonstrates significant inhibitory activity against P-glycoprotein (P-gp) overexpressing cell lines MCF7/ADR and KBV200, with resistance indices (DRI) of 0.83 and 0.58, respectively. In an MCF-7 xenograft model, Antitumor agent-200 (at 25 mg/kg, administered intraperitoneally) achieves a 57.2% tumor growth inhibition rate. This compound is applicable for research in the field of cancer therapy.

Antitumor agent-199 (Compound 4b) is an antitumor compound exhibiting significant antiproliferative activity against various tumor cell lines. It can induce autophagy (autophagy) in cancer cells through the ATG5/ATG7 pathway, making it useful for tumor research.

Antitumor agent-202 is a stabilizer of the p53Y220C mutant, selectively inhibiting the proliferation of tumor cells carrying the p53Y220C mutation. It is applicable for research focused on cancers associated with the p53 Y220C mutation.

Antitumor agent-201 (Compound 10) is a Golgi apparatus-targeting chloride ion transport activator with an EC50 for promoting transmembrane chloride ion transport of 1.53 mol% and an IC50 against HepG2 cells of 7.13 μM. By selectively acting on the Golgi apparatus, Antitumor agent-201 disrupts chloride ion homeostasis, decreases the expression of key proteins such as GM130 and GRASP55, and alters Golgi structure and function. This process induces Golgi apparatus autophagy, triggers apoptosis in cancer cells, and causes cell cycle arrest at the G2/M phase, thereby exhibiting anticancer activity. Antitumor agent-201 is applicable for research in the field of cancer-related diseases.

Antitumor agent-190 (Compound 26) is a hexokinase 2 (Hexokinase2) inhibitor that exhibits significant antitumor activity by targeting both microtubules and hexokinase 2 (Hexokinase2), with an IC50 value of 0.764 μM against MD-MBA-231 cells. It effectively suppresses Hexokinase2 activity, resulting in the accumulation of reactive oxygen species (Reactive Oxygen Species) and disruption of mitochondrial membrane potential (MMP), thus promoting apoptosis and causing cell cycle arrest.

Antitumor agent-99 (compound 7) is a cancer-fighting substance that targets FRα/β and PCFT. It effectively inhibits R2/PCFT4 (PCFT), RT16(FRα), and D4(FRβ) cells with IC50 values of 51.46 nM, 2.53 nM, and 2.98 nM, respectively.

Antitumor agent-123 (Compound 4d) effectively inhibits various kinase targets with anticancer properties, including JAK2, JAK3, HDAC1, and HDAC6, with IC50 values of 34.6 μM for JAK2 and 2.6 μM for JAK3. In solid tumor models, Antitumor agent-123 demonstrates moderate activity.

Antitumor agent-125 is a novel platinum (IV) prodrug. It activates the mitochondria-dependent apoptosis pathway and induces ferroptosis in HCT-116/OXA cells.

Antitumor agent-126 (Compound II4) is a photoreactive anticancer compound (IC50 = 0.149) that exhibits significant near-infrared fluorescence emission at 650-760 nm. It demonstrates antiproliferative activity and induces apoptosis upon laser irradiation. This compound effectively inhibits tumor growth in mouse xenograft models when exposed to 650 nm laser light, making it valuable for cancer research.