Antitumor agent 2

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

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.

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

VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.

4-oxo Cyclophosphamide is an inactive metabolite of the alkylating agent cyclophosphamide .1,2It is formed from cyclophosphamide through a 4-hydroxycyclophosphamide intermediate by aldehyde dehydrogenases.2 1.Struck, R.F., Kirk, M.C., Mellett, L.B., et al.Urinary metabolites of the antitumor agent cyclophosphamideMol. Pharmacol.7(5)519-529(1971) 2.de Jonge, M.E., Huitema, A.D.R., Rodenhuis, S., et al.Clinical pharmacokinetics of cyclophosphamideClin. Pharmacokinet.44(11)1135-1164(2005)

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.

cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when administered at doses of 40 and 80 mg/kg, respectively.2 1.Lovejoy, K.S., Todd, R.C., Zhang, S., et al.cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospectsProc. Natl. Acad. Sci. USA105(26)8902-9807(2008) 2.Hollis, L.S., Amundsen, A.R., and Stern, E.W.Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumor agents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor)Cl]+J. Med. Chem.32128-136(1989)

LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4 6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4 6 (cdk4 6) by conjugation of cdk4 6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

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].

Acyclovir monophosphate is a potent anti-Herpes Simplex Virus (HSV) agent with antitumor activity, blocking DNA synthesis by inhibiting viral DNA polymerase and terminating viral DNA chain elongation [1] [2].

Antiproliferative agent-6 (compound 8a) is a potent antitumor compound exhibiting antiproliferative activity. It inhibits cancer cell lines HCT116, MCF-7, H460, and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50 values of 0.5 μM, 2 μM, 0.7 μM, and 3.5 μM, respectively.

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.