antimitotic

Carbendazim (Mercarzole) is a broad-spectrum benzimidazole antifungal with potential antimitotic and antineoplastic activities. Although the exact mechanism of action is unclear, carbendazim appears to binds to an unspecified site on tubulin and suppresses microtubule assembly dynamic. This results in cell cycle arrest at the G2 M phase and an induction of apoptosis.

Cycloheximide (Naramycin A) is a natural product that reversibly inhibits translation elongation, is an antimitotic compound, and is an inhibitor of DNA and protein synthesis.

A series of N-Phenylbenzylamine (Benzenemethanamine) as potential cytotoxic and antimitotic agents acting by inhibition of tubulin polymerization

Razoxane is used as an antimitotic agent with immunosuppressive properties.

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity.

3-hydroxydecanoic acid is a medium-chain fatty acid. It has a role as an antimitotic and an Escherichia coli metabolite.

CHM-1 is an inducer of apoptosis, and displays potent antitumor ability in human hepatocellular carcinoma by activation of Cdc2 kinase activity. CHM-1 inhibits tubulin polymerization in vitro and in vivo.

Indibulin (D 24851) is a synthetic small molecule with antimitotic and potential antineoplastic activities.Indibulin an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM.

Vindoline is an indole alkaloid that exhibits antimitotic activity by inhibiting microtubule assembly.

AVE-8063 is an antimitotic agent or microtubule inhibitor with potential anticancer activity.

Homopterocarpin and Pterocarpus extract offer gastroprotection against indomethacin- induced ulcer by antioxidative mechanism and the modulation of gastric homeostasis, homopterocarpin may be responsible for, or contribute to the antiulcerogenic property

Prostaglandin D2 (PGD2) is a primary enzymatic prostaglandin derived from PGH2 and is abundantly produced in the cerebrospinal fluid (CSF) by the lipocalin-type PGD synthase, and peripherally by myeloid cells such as mast cells and basophils via a hematopoietic-type PGD synthase. PGD2 is chemically unstable and presents challenges for use and analysis due to its brief in vivo half-life. Δ12-PGD2, an initial decomposition product of PGD2, acts as an intermediate in the pathway to Δ12-PGJ2, a cyclopentenone prostaglandin known for its antimitotic and carcinogenic properties. The metabolism of Δ12-PGD2 involves the addition of thiol nucleophiles, a common pathway for many cyclopentenone prostaglandins.

Nampt-IN-10 trihydrochloride (Compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor exhibiting cellular potency against A2780 and CORL23 cell lines, with IC50 values of 5 nM and 19 nM, respectively. It holds potential as a novel non-antimitotic payload for antibody-drug conjugate (ADC) [1].

Estramustine (LEO-275) is a nitrogen mustard linked to estradiol, usually as phosphate. Estramustine has been used to treat prostatic neoplasms; also has radiation protective properties. Estramustine is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone.

Epofolate is folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

DAT1 is an antimitotic and antiangiogenic that acts by binding to the colchicine binding site of tubulin.

N-Boc-Val-Dil-Dap-Doe is used in the synthesis of Dolastatin 10, a potent antimitotic peptide that inhibits tubulin polymerization.

Dov-Val-Dil-OH is a useful chemical intermediate for synthesis of auristatin-related compounds, such as Monomethyl auristatin E (MMAE), Auristatins are antimitotic agents which inhibits cell division by blocking the polymerisation of tubulin.

Guattegaumerine, a bisbenzylisoquinoline alkaloid, exhibits antimitotic, cytotoxic, and neuroprotective activities.

5HPP-33 is an microtubule-stabilizer with the properties of antiproliferative and antimitotic.

Dolastatin 10 trifluoroacetate is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have an activity to inhibit tubulin polymerization (IC50: 1.2 μM). Besides that, it

Amikhellin HCl, an antimitotic drug, is a synthetic water-soluble derivative of khellin, an alkaloid extracted from seeds of Ammi Visnaga. Amikhellin has been used so far mostly as a vasodiator. Amikhellin binds to double-stranded DNA by an intercalation process. It inhibits the DNA-polymerase from murine sarcoma leukemia virus.

Ceratamine A, an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., functions as a microtubule-stabilizing agent with cytotoxic effects against human cancer cell lines.

MMAF (MonoMethyl auristatin F), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin.

Dolastatin 10 (DLS 10) is a potent peptide with antimitotic properties, effectively inhibiting tubulin polymerization.

Nampt-IN-10 TFA (compound 4) is a phosphoribosyltransferase (NAMPT) inhibitor with cellular efficacy against A2780 (IC50: 5 nM) and CORL23 (IC50: 19 nM), and can be used as a non-antimitotic payload for ADCs.

DMU-212 is a methylated derivative of resveratrol with antimitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities. It induces mitotic arrest, apoptosis, and activation of ERK1 2 protein and has oral activity[1][2]. DMU-212 (0.3125-40 μM) inhibits the growth of human melanoma cells (A375, MeWo, Bro, M5)[1]. At concentrations of 30-50 μM over 24 hours, it upregulates cell cycle inhibitors, induces apoptosis, and activates ERK in A375 cells[1]. DMU-212 also induces G2 M arrest and apoptosis in cancer cells[1]. In a xenograft model of human ovarian cancer with six-week-old SCID female mice (20-24 g), DMU-212 (50 mg kg, administered orally three times a week for 14 days) inhibits tumor growth[2]. [1]. Vasilis Pericles Androutsopoulos, et al. Activation of ERK1 2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4. [2]. Hanna Piotrowska, et al. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400.

Tasidotin hydrochloride, a peptide analog of the antimitotic depsipeptide dolastatin 15, is an inhibitor of microtubule assembly and microtubule dynamics.

SSE1806, a podophyllotoxin derivative (a natural antimitotic agent), functions as a microtubule/tubulin inhibitor, exhibiting potent anticancer and antiproliferative properties. It demonstrates a GI50 for inhibiting cancer cell growth between 1.29-21.15 μM. This compound induces mitotic disruption and G2/M phase arrest, upregulates p53 expression, and suppresses the growth of colon cancer organoids. Notably, SSE1806 can counteract multidrug resistance in cell lines that overexpress MDR-1 [1].

E7974 is an analog of the sponge-derived anti-microtubule tripeptide hemiasterlin with antimitotic and potential antineoplastic activities. Hemiasterlin analog E7974 binds to the Vinca domain on tubulin, resulting in inhibition of tubulin polymerization and microtubule assembly; depolymerization of exsiting microtubules; inhibition of mitosis; and inhibition of cellular proliferation. This agent may have more affinity for the beta-3 tubulin isotype. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Dolastatin 15, a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the anti-tubulin agent Dolastatin 10. Dolastatin 15 can be used as an ADC cytotoxin and it induces cell cycle arrest and apoptosis in m

(-)-beta-Peltatin has antimitotic, and antineoplastic activities.

Estramustine phosphate sodium (Ro 21-8837 001) is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2 M phase of the cell cycle.

Batabulin (T138067) is an antitumor compound that binds covalently and selectively to a subset of the β-tubulin isotypes, disrupting microtubule polymerization. This disruption affects cell morphology, induces cell-cycle arrest, and ultimately leads to apoptotic cell death.

TAS-119 (TAS-2104) is an orally available, selective and potent inhibitor of Aurora A with an IC50 of 1.0 nM.TAS-119 also inhibits Aurora B with an IC50 of 95 nM.TAS-119 has a higher affinity for Aurora A than for Aurora B.TAS-119 exhibits potent antitumor activity and potential antimitotic activity. TAS-119 has potent anti-tumor activity and potential anti-mitotic activity.

OUN10989, an analogue compound of LP-261, is a Potent Antimitotic Agent. OUN10989 exhibited potent inhibition of mitosis at the G2/M stage. OUN10989 was first reported in J. Med. Chem 54(1), 179-200; 2011 (compound 7). This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

Amikhelline is an antimitotic drug. It acts as a DNA intercalator and inhibits DNA polymerase.

1. Santalol has good antibacterial, anti-oxidation and anti-tumor activities. 2. α-Santalol is a potent antimitotic agent induced by interference with microtubule assembly. 3. α-Santalol shows a significant antifungal effect against a dermatophytic fungus

Maytansinoid B, an ADC cytotoxin, conjugates with antibodies to create antibody-drug conjugates (ADCs). This antimitotic agent binds to tubulin, inhibiting microtubule assembly, and induces G2/M arrest in the cell cycle, leading to apoptosis [1] [2].

Wikstrol A, a potent antifungal, antimitotic, and anti-HIV-1 agent, demonstrates significant effects across various biological targets. It induces morphological deformation in P. oryzae mycelia, with a minimum morphological deformation concentration (MMDC) of 70.1 µM and inhibits microtubule polymerization, evidenced by an IC50 value of 131 µM. Additionally, Wikstrol A exhibits anti-HIV-1 activity with an IC50 value of 67.8 µM.

Antitumor agent-88, a competitive inhibitor of CYP1A1 (K i: 1.4 μM), demonstrates significant antimitotic activity by arresting cells in the G2/M phase and disrupting the microtubule network and cytoskeleton in CYP1A1-expressing breast cancer cells.

Trimethylcolchicinic acid methyl ether (HAN 76504), an antimitotic agent, blocks microtubule assembly by attaching to tubulin and inhibiting its polymerization. It enhances tubulin's intrinsic GTPase activity, induces apoptosis across various normal and tumor cell lines, and activates the JNK/SAPK pathway. Currently unnamed, it is referred to by a provisional code name in line with MedKoo Chemical Nomenclature (https://www.medkoo.com/page/naming) for ease of communication.

Scoulerine is an inhibitor of ß-site amyloid precursor protein cleaving enzyme 1(BACE1). Scoulerine a potent antimitotic compound that inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.