Antitumor agent 3

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

VK3-OCH3 (2-[(2-Methoxy)ethylthio]-3-methyl-1,4-na) is a selective antitumor agent via heme oxygenase (HO-1) related mechanisms; Vitamine K3 analogue.

Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. It also induces apoptosis and inhibits aminopeptidase M, aminopeptidase N, and leucine aminopeptidase, as well as MMP-1, MMP-3, MMP-8, MMP-9, and meprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin exhibits antiproliferative and antitumor activities [1][2][3][4][5].

Duocarmycin A, an antitumor antibiotic, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results in HLC-2 cells typically apoptotic changes.

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

Skp2 inhibitor 3 (E35), a potent antitumor agent, acts as a robust inhibitor of S-phase kinase-associated protein 2 (SKP2) with an IC50 of 4.86 μM for Skp2-Cks1 binding. It significantly suppresses colony formation and migration, while inducing cell cycle arrest in the S-phase.

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.

Phosphoramide mustard cyclohexanamine is the active metabolite of cyclophosphamide, an alkylating agent that cross-links DNA strands, organizes cell division and causes cell death, and has antitumor activity.

Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. It exhibits antitumor activity and can reduce atherosclerosis. This compound is a nonselective inhibitor of COX with IC50 values of 6.5 μM for COX-1 and 13.5 μM for COX-2 [1] [2] [3] [4].

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.

Antitumor agent-77 inhibits the growth and migration of cancer cells and has anticancer effects. antitumor agent-77 inhibits GPx-4 and enhances COX2-induced iron sagging. antitumor agent-77 activates the intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) in tumor cells and prevents tumor cell epithelialization. Antitumor agent-77 activates the tumour cell intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and blocks the epithelial mesenchymal transition (EMT) process.

Antitumor agent-54 (Compound C11) is a 14-3-3η protein inhibitor (KD: 35 μM). antitumor agent-54 inhibits several typical human hepatocellular carcinoma cell lines. antitumor agent-54 blocks the cell cycle in the G1-S phase and induces apoptosis, showing good metabolic stability. It exhibits good metabolic stability.

Antitumor agent-72 (compound 6w) is a potent anticancer agent that induces apoptosis by activating caspase-3 and cleaving PARP, making it valuable for cancer research [1].

Antitumor agent-78 inhibits GPx-4 and elevates COX2, leading to ferroptosis. antitumor agent-78 activates the tumor cell intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and inhibits the epithelial mesenchymal transition (EMT) process in tumor cells. Antitumor agent-78 exhibits antitumor effects and inhibits the growth and migration of cancer cells.

Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50 IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 + - 0.08 micromol l after 24 h) than As(2)O(3) (IC50 = 1.60 + - 0.23 micromol l after 24 h) or melarsoprol (IC50 = 1.44 + - 0.08 micromol l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration.

Neuroinflammatory-IN-3 is a tubulin inhibitor that serves as both an anti-neuroinflammatory agent and a potent antitumor agent by inhibiting tubulin polymerization.

KRAS G12D Inhibitor 3 TFA, exhibiting an inhibitory concentration (IC50) of less than 500 nM, is effective as an antitumor agent.

Antitumor agent-61 (Compound 9b), an Irinotecan (Ir) derivative, demonstrates potent anticancer activity with IC50 values ranging from 0.92 to 3.23 μM against six human cancer cell lines: SK-OV-3, SK-OV-3 CDDP, U2OS, MCF-7, A549, and MG-63, and specifically induces apoptosis in SK-OV-3 cells via mitochondrial pathways [1].

Azurin p28 peptide, a tumor-penetrating antitumor agent, stabilizes p53 by reducing its proteasomal degradation via the formation of a p28:p53 complex. It elicits apoptosis or cell cycle arrest and suppresses the growth of p53-positive tumors. Additionally, the peptide exhibits antiangiogenic properties by inhibiting the phosphorylation of VEGFR-2, FAK, and Akt [1] [2] [3].

Antitumor agent-67 (compound 3), a potent antitumor agent, exhibits highly selective toxicity toward cancer cells while sparing normal cells. This compound can be activated by NQO1 to effectively release podophyllotoxin, thereby killing tumor cells. In HepG2 xenograft models, Antitumor agent-67 significantly inhibits cancer growth with minimal toxicity [1].

Antitumor agent-149 (Compound 3), an analogue of Echinomycin, inhibits HIF-1α-mediated transcription, induces cancer cell apoptosis, and suppresses tumor growth in the SW620 xenograft mice model [1].

Nitracrine (dihydrochloride hydrate), a 1-nitroacridine derivative, inhibits RNA synthesis, reversibly binds to DNA, and forms covalent adducts with DNA in vivo. It is a potent hypoxia-selective and antitumor agent in vitro, exhibiting cytotoxicity towards most cells [1] [2] [3].

Antitumor agent-182 (Compound 12a) reduces mitochondrial membrane potential (MMP) and elevates levels of reactive oxygen species (ROS). It impedes the cell cycle during the G0 G1 phase and induces apoptosis in HeLa cells. Furthermore, Antitumor agent-182 inhibits the proliferation of HeLa, PC-3, and HCT-15 cells with IC50 values of 8.83, 10.07, and 7.84 μM, respectively.