antitumor agent-2

Antitumor agent-2 has anti-inflammatory and anti-tumor activity and can be used to study cancer.

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-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-21 (TRX818) is an orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities.

Antitumor agent-28 is a compound that specifically targets and inhibits the activity of the ataxia telangiectasia mutated (ATM) kinase. By doing so, it effectively impedes the progression of ATM-mediated diseases and demonstrates significant anti-cancer activity.

Antitumor agent-23 exhibits potent antitumoral activity, as demonstrated by its GI50 values of 38, 48, 5, 27, 80, and 28 nM against the lymphoma cell lines GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI respectively.

Antitumor agent-29 is a hepatocyte-targeting prodrug with demonstrated efficacy and minimal toxicity in anticancer applications.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

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.

2'-Deoxy-2'-fluoro-beta-D-arabinoguanosine is a purine nucleoside analog with a broad spectrum of antitumor activity, targeting malignant tumors of the inert lymphatic system and inducing apoptosis. The anticancer mechanism of 2'-Deoxy-2'-fluoro-beta-D-arabinoguanosine is dependent on the inhibition of DNA synthesis.

4-(Benzo[d]oxazol-2-yl)aniline is a potent antitumor agent with inhibitory activity against mammary carcinoma cell lines [1].

JI051 is an antitumor agent that interacts with the cancer-associated protein chaperone prohibitin 2 (PHB2) to induce cell cycle arrest by inhibiting the transcription of the Notch downstream effector gene, Hes1, and inhibits the proliferation of HEK293 cells and pancreatic cancer cells.

Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

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].

CB 300919 is a quinazoline-based antitumor agent exhibiting high activity against CH1 human ovarian tumor xenografts, with continuous exposure (96 h) resulting in a growth inhibition (IC50: 2 nM).

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.

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.

2-Aminohexadecanoic acid is a bioactive compound noted for its tumor growth inhibitory activity. Research indicates that it targets basic proteins, disrupting the proliferation of tumor cells. The primary application of 2-Aminohexadecanoic acid is its potential use as an antitumor agent.

Myoseverin B is a microtubule assembly inhibitor that impedes tubulin polymerization (IC50 = 2 μM) and generally exhibits low cytotoxicity across most cell types. It is utilized in antitumor agent research.

LC3B recruiter 2 (34R) is an LC3B recruiting agent incorporated into the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), with a direct binding affinity for LC3B. It connects via a linker to the CDK9 inhibitor SNS-032, creating an ATTEC capable of targeting and degrading the CDK9 and Cyclin T1 complex, while also inhibiting them. Consequently, LC3B recruiter 2 exerts its function through an LC3B-dependent autophagy-lysosome pathway, interfering with the cancer cell cycle progression, thereby demonstrating antitumor activity.

[Ru(phen)2(HMPIP)](PF6)2 (Compound 6A) is an antitumor agent that inhibits the proliferation and migration of liver cancer cells (HepG2), while inducing apoptosis, autophagy, cell cycle arrest, and ferroptosis. It enhances antitumor activity by stimulating immune response, leading to an increase in CD8+ T cells.

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.

Physapubenolide is natural cytotoxic withanolide antitumor agent. Physapubenolide induces apoptosis by decreasing mitochondrial membrane potential and elevating the Bax/Bcl-2 protein expression ratio.