antitumor effects

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

Amygdalin (Laetrile) has antifibrotic, antitumor, anti-inflammatory and analgesic effects, amygdalin joint HSYA could inhibit the degeneration of the endplate chondrocytes derived from intervertebral discs of rats induced by IL-1beta and better than the single use of Amygdalin or HSYA. Amygdalin induces apoptotic cell death in human DU145 and LNCaP prostate cancer cells by caspase-3 activation through down-regulation of Bcl-2 and up-regulation of Bax.

2-Amino-2-dichlorobenzophenone is an aromatic natural compound that has been used to study the effects of various compounds on cell metabolism, protein synthesis and enzyme activity. It has also been used in the synthesis of drugs, such as antitumor drugs and anti-inflammatory agents.

Genistein (NPI 031L) is a naturally occurring soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor, antioxidant, and anthelmintic properties, and also produces estrogen-like effects in the body.

N-[2-nitro-4-(trifluoromethyl)phenyl]piperazine is a biologically active compound belonging to the piperazine group. It is an important synthetic intermediate used in the preparation of a wide range of drugs, agrochemicals and other chemicals. It is considered an inhibitor of certain enzymes involved in drug metabolism, such as cytochrome P450 enzymes, and has also been shown to have anti-inflammatory and antitumor effects.

CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC).. CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .

(Z)-Butylidenephthalide ((Z)-3-Butylidenephthalide) has antitumor and hypoglycemic effects, and can effectively inhibit the tumor growth of glioma and inhibit R-glucosidase activity.

Tegadifur (40497S) is an orally available antitumor compound with antimetabolic effects, often used with uracil and in the treatment of rectal adenocarcinoma.

IRAK4-IN-20 is a potent and orally active IRAK4 inhibitor (IC50:3.55 nM). IRAK4-IN-20, which has anti-inflammatory, antitumor and anticancer effects, is often used to treat acute respiratory distress syndrome (ARDS).

2’-Deoxy-2’-fluoro-β-D-arabinocytidine hydrochloride is a cytosine nucleoside analog with inhibitory effects on DNA methyltransferase , with potential antimetabolic and antitumor activity.

FT001 is a potent, selective and orally available inhibitor of BET Bromodomain with antitumor activity. FT001 inhibited the expression of MYC with the IC50 value of 0.46 μM). FT001 has potent antiproliferative effects against MV-4-11 and demonstrates significant MYC mRNA suppression both in vitro and in vivo.

Cholesteryl Hemisuccinate Tris Salt is an acidic cholesteryl ester with hepatoprotective and anticancer activity.Cholesteryl hemisuccinate is a membrane stabilizer in dipalmitoylphosphatidylcholine liposomes containing Chaikosaponin-d, which enhances the anticancer efficacy of cisplatin.Cholesteryl hemisuccinate possesses antitumor activity, inhibits tumor Cholesteryl hemisuccinate has antitumor activity, inhibits tumor growth, inhibits the hepatotoxicity of acetaminophen (AAP) and prevents AAP-induced apoptosis of hepatocytes.Cholesteryl hemisuccinate protects rodents against the toxic effects of acetaminophen, adriamycin, carbon tetrachloride, chloroform, and galactosamine.

5-amino-1-[4-(trifluoromethyl)phenyl]-1H-pyrazole-4-carbonitrile is a compound used as a molecular structural unit and is considered to be an inhibitor of enzymes such as COX-2, 5-LOX, etc., and possesses a wide range of biochemical and physiological effects including antitumor activity, anti-inflammatory effects and antioxidant activity.

Hentriacontane is a natural product.

CPS-11 (N-(Hydroxymethyl)thalidomide) is a Thalidomide analogue with significant antitumor activity, exhibiting a broader and more potent effect on the MM (multiple myeloma) cell line.

KW-2450 Formate is an IGF-1R/IR tyrosine kinase inhibitor with antitumor effects that acts through inhibition of Aurora A and B kinases.KW-2450 Formate inhibits the growth of TNBC xenografts and induces tetraploid accumulation.

C-Reactive Protein (CRP) 174-185 acetate is an acute phase serum protein synthesized in response to inflammatory cytokines, produces antitumor effects in animals. The fragment CRP (174-185) (RS-83277) shows similar activity by significantly enhancing the

Antitumor agent-87 is a potent compound exhibiting high antitumoral activity, with a Ki value of 0.23 µM for CYP1A1. It demonstrates antiproliferative effects and induces cell cycle arrest at the G2 M phase, underscoring its effectiveness as an antitumor agent.

Laprafylline is a xanthine compound with inhibitory effects on bronchoconstriction in vivo and antitumor activity.Laprafylline acts as a competitive serotonergic antagonist at low concentrations, and inhibits constriction induced by hist at high difficulties.

3-hydroxy-3-phenylpentanamide is a chiral compound belonging to the class of beta-hydroxyamides. In neurology, it has been shown to have neuroprotective effects against ischemic brain injury and cerebral hemorrhage. In psychiatry, it has been studied as a potential treatment for anxiety, depression and addiction. In oncology, it has been shown to have antitumor activity by inducing apoptosis and inhibiting tumor growth.

Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory effects on pHER2 and EGF.

Girinimbine (Girinimbin) is a carbazole alkaloid isolated from the plants M. koenigii, M. koenigii, and Murraya koenigii. Girinimbine exhibits a wide range of biological effects, including apoptosis, antitrypanosomal, antiplatelet, antimicrobial, anti-inflammatory, antioxidant, and antitumor activities.

GCN2-IN-7 is a selective, orally active general control nonderepressible 2 (GCN2) inhibitor with an IC50 value of 5 nM that exhibits antitumor effects in vivo.

Mifamurtide is a drug against osteosarcoma, is an immunomodulator with antitumor effects.

Syringin (eleutheroside-b) is a compound with antitumor, antiproliferative, immunomodulatory and platelet aggregation inhibiting effects.

Salvigenin is a potent hMAO-A inhibitor, has neuroprotective, antitumor and immunomodulatory effects.

Isopsoralenoside shows estrogen-like, osteoblastic proliferation accelerating, antitumor, and antibacterial effects.

Punicalagin is a major ellagitannin found in pomegranates that is reported to produce antioxidant, anti-inflammatory, and anticancer effects. It has been shown to prevent high-fat diet-induced obesity-associated accumulation of cardiac triglyceride and ch

1. Morusin (Mulberrochromene) possesses antitumor effects of cell lines including HT-29, A549, MCF-7, and MDA-MB-231, through suppressing STAT3 and NFκB attenuation mediated apoptosis induction. 2. Morusin possesses anti-oxidant and anti-inflammatory effects.

Butyrolactone I (Olomoucin) is an ATP-competitive inhibitor of CDK and cdc2 kinase family. Butyrolactone I shows antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines.

1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

Psoralenoside is a natural product isolated from the fruits of Psoralea corylifolia, shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630/624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Valepotriate (Valtrate) fraction can have sedative effects and affect behavioral parameters related to recognition memory. Valepotriates, a new class of cytotoxic and antitumor agents, they are very potent cytotoxic agents for the HTC hepatoma cells. Valepotriates may have a potential anxiolytic effect on the psychic symptoms of anxiety.

Cedrelone is a citrulline analog and a phenazine biosynthesis-like domain protein (PBLD) activator.Cedrelone induces apoptosis in cancer cells.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone has insecticidal activity, inhibiting the growth of arrowhead venom of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus). Cedrelone has insecticidal activity, inhibiting the growth of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus).Cedrelone has antitumor effects and exhibits significant cytotoxicity against cancer cell lines such as -60, SMMC-7721, A-549, MCF-7, and SW480.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone is a very potent inducer of apoptosis, leading to cell cycle arrest.

Imidazole ketone erastin (IKE) is an ferroptosis inducer with inhibitory effects on system Xc-cystine/glutamate transporter proteins. Imidazole ketone erastin has antitumor activity and induces glutathione depletion and lipid peroxidation.

Millepachine is a natural product found in the Chinese herbal medicine with strong antitumor effects against numerous human cancer cells.

Wushanicaritin is a natural product isolated from the traditional Chinese medicine Epimedium plants, with antitumor effects and anti-inflammatory property.

Isodeoxyelephantopin exerts antitumor effects on several cancer cells by inducing apoptosis , cell cycle arrest , and inhibiting proliferation. It enhances apoptosis and inhibit invasion and osteoclastogenesis by inhibiting NF-kappaB activation and NF-kap

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand and telomerase inhibitor that exhibits antitumor effects in osteosarcoma cell lines.

Aromatase-IN-2 has anti-inflammatory, antitumor and antiasthmatic effects.

Hypocrellin A is PKC inhibitor, has light-induced antitumor,antifungal and antiviral activities, it also exerts immunomodulatory effects on MHC-restricted presentation of antigen.

SZL P1-41, a skp2 inhibitor, can prevent assembly of Skp2-Skp1 complexes. It selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the activity of other SCF complexes. It also inhibits Skp2-mediated p27 and Akt ubiquitination in vivo and in vitro. It suppresses the survival of Y cells and Y stem cells by triggering cell senescence and inhibiting glycolysis. It exhibits antitumor effects in multiple animal models and Y cell lines.

N-(p-Coumaroyl) Serotonin, a polyphenol isolated from the seeds of safflower, exhibits antioxidant, cardioprotective effects after ischemia, and antitumor activity. It may improve vascular distensibility and reduce cardiovascular risk. N-(p-Coumaroyl) Serotonin ameliorates atherosclerosis and distensibility of the aortic wall in vivo, and is commonly used in atherosclerosis research.

HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with a Ki of 60 nM for HDAC2 and 30 nM for HDAC6, exhibiting antitumor effects.

SphK1&2-IN-1, a sphingosine kinase inhibitor, exhibits anti-inflammatory, antitumor, and hemostatic properties.

γ-Tocotrienol (Plastochromanol) is one of the four types of tocotrienol, a type of vitamin E. Itl is also a radioprotector, antioxidant. It shows antitumor and antihypertensive effects in vivo.

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

Gilteritinib hemifumarate (ASP2215 hemifumarate) is a potent ATP-competitive dual FLT3 (IC50: 0.29 nM) and AXL (IC50: 0.73 nM) inhibitor for the treatment of relapsed or refractory FLT3 mutant AML.