cytostatic

Cytembena is a cytostatic and a carcinogenic compound that may increase the incidence of fibroadenomas.Cytembena broadly inhibits DNA biosynthesis.

1. Betulonic acid (Liquidambaric acid) amide stimulated the regenerative response in hepatocytes under conditions of combined toxic exposure and promoted recovery of their qualitative and quantitative characteristics, which was accompanied by a significant decrease in the severity of liver fibrosis and the absence of cirrhotic transformation of the liver. 2. Betulonic acid derivatives have a promising cytostatic activity in vitro and could be used as potential leads for the development of new type of anti-cancer agents. 3. Betulonic acid has antiholestatic effects in mice.

Carboxyamidotriazole Orotate (L-651582 Orotate) is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor that in vitro has been shown to possess antileukaemic activities. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory, and antiangiogenic effects.

Benin (Butocine) is an effective cytostatic drug used for the treatment of generalized carcinoma of the breast.

Santamarine has significant anticancer activity, can inhibit L1210 cells because of its cytotoxic,cytostatic and blocking mitosis and reducing uptake of thymidine. Santamarine and reynosin show bactericidal activity against clinical strains of Mycobacterium tuberculosis.

Cyclosporin U (SMP0V32C6L) is a cytostatic agent critical for the prevention of organ transplant rejection [1].

Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herboxidiene (0.05 μM) inhibits HIF-1α mRNA splicing and reduces HIF-1α protein levels in HepG2 cells grown under hypoxic conditions. It also inhibits splicing of p27Kip mRNA in HeLa cells in a concentration-dependent manner via interaction with the SAP155 subunit of the SF3b complex.[2] Herboxidiene (0.1 and 1 μM) increases LDL receptor promoter-driven transcription in a cell-based reporter assay.[5] It also exhibits herbicidal activity against wild buckwheat, morning glory, maize, hemp sesbania, and rapeseed when applied at 0.069 kg/hectare.[1]

Vinformide is a potent cytostatic agent.

Loliolid is a germination inhibitor, and a repellent for ants (Atta cephalotes).It has cytostatic activity against carcnoma and leukaemia cells.

Tolytoxin is a cytostatic, antifungal macrolide produced by blue-green algae of the genus Scytonema, is a potent, reversible inhibitor of cytokinesis in cultured mammalian cells

Tezacitabine is a cytostatic and cytotoxic antimetabolite. Tezacitabine is a nucleoside analogue characterized by a dual mechanism of action. Tezacitabine irreversibly inhibits ribonucleotide reductase and can be incorporated into DNA during replication or repair, resulting in DNA chain termination. Tezacitabine blocks tumor cells in G1 and S phases of the cell cycle and induces apoptotic cell death. Tezacitabine has the potential to treat leukemia and solid tumors[1][2].

Dihydrochlamydocin, an inhibitor of histone deacetylases (HDAC), exhibits potent cytostatic activity against mastocytoma cells.

Eupatorin has antiproliferative and antiangiogenic effects. Eupatorin has antiproliferative and cytostatic effects on MDA-MB-468 human breast cancer cells due to CYP1-mediated metabolism. Eupatorin-induced cell death is mediated by both the extrinsic and

Cycloleucine is an antagonist of NMDA receptor associated glycine receptor with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of S-adenosyl-methionine mediated methylation with anxiolytic and cytostatic effects.

YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor, with an IC50 of 1-5 μM for PAD4. Compared with Cl-amidine, YW3-56 shows >60-fold increase in cell growth inhibition efficacy (IC50 about 2.5 μM) but only 5-fold increase in PAD4 inhibition (IC sub>50 about 1-5 μM). At 2-4 μM concentrations, YW3-56 displays mainly cytostatic effects by slowing cell division, whereas at higher concentrations, it exerts cytotoxic effects by altering cell morphology and killing cells[1]. [1]. Wang Y, et al. Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and t he mammalian target of rapamycin complex 1 activity. J Biol Chem. 2012 Jul 27;287(31):25941-53.

Alestramustine is a cytostatic antineoplastic agent. The drug, via its active metabolites, binds to microtubule-associated proteins and β-tubulin and interferes with microtubule function, thereby suppressing cell division. Due to its estrogen moiety, Ales

Carboxyamidotriazole is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. It shows anti-inflammatory, anti-tumor, and antiangiogenic effects.

(–)-Voacangarine, an indole alkaloid isolated from V. africana, exhibits cytotoxicity towards various cell lines including HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 values of 20 µg/ml. Additionally, it demonstrates cytostatic effects on wild-type S. cerevisiae and is cytotoxic to Δrad3-e5 and Δrad6-1 mutant strains of S. cerevisiae, which have defects in DNA strand break repair and the mutagenic repair pathway, respectively.

Pinafide is a rodenticide and anti-protozoal agent. Pinafide shows strong cytostatic activity against both HeLa and KB cells and is moderately toxic to both mice and rats. It has been proved active against experimental tumors and shown to be inhibitor of two DNA viruses. Pinafide blocks cell growth by inhibiting DNA and RNA synthesis. It has been shown to bind to double-helical DNA by intercalation. Pinafide inhibited the activity of M. tuberculosis NAD⁺-dependent DNA ligase A at concentrations of 50 uM. At the chemical screening was found that pinafide inhibited B-Myb transcriptional activity in luciferase assays. The cross placental-barrier studies showed that 3H-pinafide was present in the 14-day fetuses.

SLLN-15 is an oral active, selective and potent enhancer of autophagy. SLLN-15 activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC) [1].

AL-8417 is an enzyme inhibitor. It acting as an antioxidant, anti-inflammatory, and cytostatic agent. It also has the ability to suppress vitrectomy-induced posterior lens fiber changes.

α-D-Glucose-1-phosphate disodium hydrate serves multiple roles in medical and biochemical applications, including as a precursor in the synthesis of glucuronic acid, a cytostatic compound crucial for cardiopathic therapy, an antibiotic, an immunosuppressive agent, and a component in circulatory system therapy [1].

Acid Ceramidase-IN-2 (compound 1), an acid ceramidase inhibitor, exhibits potentially antiproliferative and cytostatic effects. This compound is of interest due to the overexpression of human acid ceramidase in prostate cancer cells, suggesting its potential anti-tumor efficacy. Furthermore, the hydrolysis of Acid Ceramidase-IN-2 can be inhibited by 3 a-ketoamides: GT85, GT98, and GT99 in vitro [1].

KCG 1 is a keto-C-glycoside drug with antiproliferative and cytotoxic properties on tumor cells. KCG1 was 25-125 times more cytostatic on epithelial cells than on lymphoma.

Benfluron Hydrochloride is an inhibitor of HIV-1 Rev function which also acts as a cytostatic agent with substantial antiretroviral activity.