antitumor agent-4

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

Antitumor agent-43 (Compound 4B) 是一种有效的抗肿瘤剂，可诱导细胞周期阻滞在G2 M 期。Antitumor agent-43对 T-24 细胞的IC50值为0.5 μM。

Antitumor agent-44 (Compound 5n) elicits potent antitumor effects by inducing disruption of mitochondrial homeostasis, cell cycle arrest, and apoptosis in human adenocarcinoma cells. Moreover, Antitumor agent-44 demonstrates significant anti-tumor activity in a lung cancer cell xenograft mice model [1].

Antitumor agent-45 对 c-Met 表达具有抑制作用，能够将 A549 细胞的细胞阻滞在 G0 G1 和 G2 M 期，并诱导其凋亡。

Antitumor agent-42 能够抑制微管多聚和 NO 释放，表现出抗血管生成、抑制集落形成和诱导凋亡作用。

Antitumor agent-46 是一种抗肿瘤剂。Antitumor agent-46 对 MCF-7 细胞具有明显更高的抗增殖活性，IC50值为 2.08 µM。

Antitumor agent-47 是一种具有抗肿瘤活性的水飞蓟宾衍生物。Antitumor agent-47 对 NCI-H1299 和 HT29 细胞具有细胞毒活性，IC50值分别为 8.07 µM 和 6.27 µM。

Antitumor agent-48 是一种具有抗肿瘤活性的 2,3-dehydrosilybin 衍生物。Antitumor agent-48 对 MCF-7、NCI-H1299、HepG2 和 HT29 细胞具有细胞毒活性，IC50值分别为 8.06 µM、13.1 µM、16.51 µM 和 12.44 µM。

Antitumor agent-41 (compound N-12)，一种具有卓越抗迁移及抗侵袭能力的抗肿瘤剂。通过坏死和炎症通路实现其抗肿瘤作用。

Antitumor agent-49 (Compound 10) 是一款 Harmine 和呋喃杂化的衍生物，带有 NO 供体且表现出抗肿瘤特性。该化合物对 HepG2 细胞线展现出显著的细胞毒性，其 IC50 值为 1.79 µM，并且能在体外产生大量的 NO。

Antitumor agent-40为一种抗癌研究用药物。

4-(Benzo[d]oxazol-2-yl)aniline 是一种有效的抗肿瘤剂，对乳腺癌细胞系具有抑制活性。

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 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].

Desacetylvinblastine (4-Desacetylvinblastine) 是长春碱的关键代谢产物和强效细胞毒性剂。虽然 Desacetylvinblastine 自身的抗肿瘤效果不理想，但在与特定共轭物结合时能够展现出显著的抗肿瘤活性。

Antitumor agent-198 (Compound A3) 在头颈部鳞状细胞癌 (HNSCC) 细胞中展现出细胞毒性，能够抑制 CAL27、HN6、HN30、SCC9 和 SCC25 细胞的增殖，IC50范围为 4 nM-77 nM。它还能够抑制 HNSCC 细胞的迁移，阻滞细胞周期并诱导细胞凋亡 (apoptosis)。

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].

Loxoprofen sodium dihydrate 是一种非甾体类口服抗炎药，具有镇痛和解热作用。Loxoprofen sodium dihydrate 显示出抗肿瘤活性，并且可减少动脉粥样硬化。Loxoprofen sodium dihydrate 是COX 的非选择性抑制剂，对 COX-1 和 COX-2 的IC50值分别为 6.5 和 13.5 μM。

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

Antitumor agent-77 对癌细胞的生长和迁移具有抑制作用，具有抗癌作用。Antitumor agent-77 能够抑制 GPx-4 和提高 COX2 引发铁下垂。Antitumor agent-77 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，阻碍肿瘤细胞上皮间质转化 (EMT) 过程。

Antitumor agent-78 能够抑制 GPx-4 和升高 COX2 ，进而导致铁下垂 (ferroptosis)。Antitumor agent-78 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，抑制肿瘤细胞上皮间质转化 (EMT) 过程。Antitumor agent-78 表现出抗肿瘤效果，并能够抑制癌细胞的生长和迁移。

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.