antitumor agent 4

Antitumor agent-4 is a butenylphenyl phosphate derivative, is an agent of mammary cancer and anovulatory sterility.

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

Fulvene-5 is a chemical compound that exhibits antitumor activity. It functions as a potent inhibitor of NADPH oxidase 4 (NOX4) and possesses antioxidant properties. Additionally, Fulvene-5 acts as a reactive oxygen species (ROS) modifying agent and a powerful radioprotector.

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].

Desacetylvinblastine (4-Desacetylvinblastine) is a primary metabolite of vinblastine and functions as a cytotoxic agent. While its antitumor efficacy is limited when used alone, it can exhibit significant antitumor activity when involved as part of specific conjugates.

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.

4'-epi-Daunorubicin is the semisynthetic precursor to Epirubicin and functions as an antitumor agent.

Antitumor agent-129 (Compound 68) is a derivative of thiazolidine-4-thione and an inhibitor of osteosarcoma (OS), with an IC50 value of 0.217 μM against OS cell activity. It has a half-life of 73.8 minutes in mouse liver microsomes and exhibits favorable pharmacokinetic properties with an in vivo bioavailability (F) of 115% following intraperitoneal administration. Antitumor agent-129 is a potential candidate for OS research.

KRN7000 analog 1 stimulates a strong Th1-biased immune response by inducing interferon-γ (IFN-γ) and reducing interleukin-4 (IL-4). This compound shows potential as an antitumor agent and vaccine adjuvant.

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)

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].

Antitumor agent-66 (Compound 4) is a derivative of (-)-cleistenolide, exhibiting potential as a research tool for cancer diseases [1].

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-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.

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).

APTO-253, also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.

APTO-253 isomer is an isomer of APTO-253 with the Fluoro-atom in 6-position. APTO-253 also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.