antitumor agent-19

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-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-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-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.

3CPLro-IN-1 (compound A17) is a potent, orally active inhibitor of SARS-CoV-2 3-Chymotrypsin-like cysteine protease (3CLpro) with an IC50 of 5.65 μM, making it an attractive drug target against COVID-19 and also considered an antitumor agent-51.