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

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.

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.

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.

Antitumor agent-119 (compound 13K), a 2-benzoxazolyl hydrazone derivative, exhibits anticancer capabilities by impeding the proliferation of Burkitt, CCRF-CEM, HeLa, and HT-29 cells, with respective IC50 values of 30 nM, 140 nM, 100 nM, and 40 nM [1].

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

Neamine, a broad-spectrum aminoglycoside antibiotic derived from Neomycin, exhibits potent antibacterial, antitumor, and neuroprotective activities. As an anti-angiogenesis agent, it specifically targets angiogenin [1] [2].

FAP-2286 is a peptidic macrocycle that binds to the fibroblast activation protein (FAP) and is linked to the chelator DOTA, facilitating its role as a tumor imaging agent in positron emission tomography (PET) research. Exhibiting strong affinity for the human FAP protein with a dissociation constant (Kd) of 1.1 nM, FAP-2286 demonstrates significant antitumor activity, as referenced in [1] [2].

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)

MC-betaglucuronide-MMAE-2 is an ADC (antibody-drug conjugate) agent-linker conjugate that exhibits potent antitumor activity; it consists of MMAE (a tubulin polymerization inhibitor) connected through the cleavable linker MC-betaglucuronide.

Shishijimicin A, a novel antitumor agent isolated from the ascidian Didemnum proliferum, exhibits highly potent cytotoxicities and demonstrates considerable anti-tumor activity [1] [2]. This compound also serves as a click chemistry reagent due to its alkyne group, enabling it to partake in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

Cantuzumab ravtansine (IMGN242; huC242-DM4), an antibody-drug conjugate (ADC), consists of the humanized monoclonal antibody huC242 covalently bonded through a disulfide linkage to the cytotoxic agent DM4 (DM4). This compound demonstrates extensive antitumor effectiveness across various CanAg-positive human tumor xenografts [1] [2].

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 is an apoptosis inducer. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase, it also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].

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].

Duocarmycin analog-2 is a potent DNA alkylating agent that exhibits antitumor effects and can be used in the synthesis of immunocouplers.

SK-575 is a degradation agent targeting protein-hydrolyzed PARP1 chimera with anticancer and antitumor activity.SK-575 effectively inhibits the growth of cancer cells harboring BRCA1/2 mutations and selectively induces PARP1 degradation in cancer cells.

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.

STA-9584 is a potent vascular disrupting agent, which exhibits potent antitumor activity by selectively targeting microvasculature at both the center and periphery of tumors. In vitro, 2-methoxy-5-(5-(3,4,5-trimethoxyphenyl)isoxazol-4-yl)aniline (STA-9122) (active metabolite of STA-9584 ) displayed increased potency relative to other tubulin-binding agents and was highly cytotoxic to tumor cells. STA-9584 induced significant tumor regressions in prostate and breast xenograft models in vivo and, in an aggressive syngeneic model, demonstrated superior tumor growth inhibition and a positive therapeutic index relative to combretastatin A-4 phosphate (CA4P).

Antiproliferative agent-6 (compound 8a) is a potent antitumor compound. Antiproliferative agent-6 shows antiproliferative activity. Antiproliferative agent-6 inhibits cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI 50 s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively.

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-37 exhibits potent anti-proliferative and anti-metastatic effects. antitumor agent-37 induces severe DNA damage, leading to high expression of γ-H2AX and p53. antitumor agent-37 induces apoptosis by exploiting the mitochondrial apoptosis pathway Bcl-2/Bax/caspase3. Antitumor agent-37 inhibits PD-L1 expression, increases CD3+ and CD8+ T-infiltrating cells in tumour tissue and significantly improves the immune response.

3CPLro-IN-1 (compound A17) is a potent, orally active inhibitor of SARS-CoV-2 3CLpro (IC50: 5.65 μM). 3-Chymotrypsin-like cysteine protease (3CLpro), a protein essential for viral replication, is an attractive drug target against COVID-19. Antitumor agent-51

Antitumor agent-36 exhibits strong anti-proliferative and anti-metastasis capabilities, causing significant DNA damage that results in elevated levels of γ-H2AX and p53. It promotes tumor cell apoptosis via the mitochondrial apoptotic pathway involving Bcl-2/Bax/caspase3 and enhances immune response by inhibiting PD-L1 expression, thereby increasing CD3+ and CD8+ T cell infiltration in tumor tissues [1].

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.

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.

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

(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC 50 s of 2.1, 0.008, and 1.2 μM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces established tumor regression[1] [2].

PI3Kγ Inhibitor 7 (compound 2) is a potent, orally active agent that selectively inhibits PI3Kγ with an IC50 of 3.42 nM and demonstrates antitumor activity [1]. It also exhibits varying inhibitory effects on other PI3K isoforms, with IC50 values of 4768 nM for PI3Kα, 878.1 nM for PI3Kβ, and 355.2 nM for PI3Kδ.

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

CB 300919 is a quinazoline-based antitumor agent with high activity in the CH1 human ovarian tumor xenograft and has continuous exposure (96 h) growth inhibition (IC50: 2 nM).

EGFR-IN-60 is an effective, orally active, safe antitumor agent. EGFR-IN-60 significantly inhibits EGFRWT (IC50: 83 nM), EGFRT790M (IC50: 26 nM), EGFRL858R (IC50: 53 nM) and JAK3 (IC50: 69 nM). IN-60 inhibited H1975 cells carrying the EGFRT790M mutation (IC50: 1.32 μM) and A431 cells overexpressing EGFRWT (IC50: 4.96 μM). EGFR-IN-60 increased the Bax/Bcl-2 ratio, which induced apoptosis induction and cell death.

Vanicoside E is an antioxidant and antitumor agent. Vanicoside E inhibits L-Tyrosine and L-DOPA with IC 50 s of 45.23 μM and 189.96 μM, respectively [1] [2] .

Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent that has analgesic and anti-pyretic properties. Loxoprofen sodium dihydrate exhibits antitumor activity which also can reduce atherosclerosis. Loxoprofen sodium dihydrate is a nonselective inhibitor of COX with IC 50 s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively [1] [2] [3] [4].

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.

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)

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.

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.