Antineoplastic

K252a, an analog of staurosporine, has been found to be a protein kinase inhibitor and exhibit antitumor activity at some extent.

Didemnin B is a cyclic depsipeptide isolated from the extract of Trididemnum solidum. It exhibits antiviral and antineoplastic effects.

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 = 20 nM), DiFi humancolon cancer cells and MDA MB-468 human breast cancer cells.

Berubicin has potential antineoplastic activity. Berubicin intercalates into DNA and interrupts topoisomerase II activity, resulting in the inhibition of DNA replication and repair, and RNA and protein synthesis.

Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.

Epothilone C is a novel microtubule inhibitor and acts as an antineoplastic agent. Epothilones are originally isolated from cellulose-degrading myxobacterium Sorangium cellulosum.

Bafilomycins are a family of macrolide antibiotics isolated from Streptomycetes sp. They exhibits antitumor, antiparasitic, immunosuppressant and antifungal activity.

Olivomycin is an antitumor antibiotic produced by Actinomyces (or Streptomyces) olivoreticuli. It is used for the treatment of testicular neoplasms, tonsillar tumors and reticulosarcoma with peripheral nodes.

Siomycin is a peptide antibiotic that interacts with the 50S ribosomal subunit and inhibits binding of factor G and aminoacyl-tRNA. It exhibits antitumor activity against certain cancer cell lines.

Stambomycin A is a macrolide antibiotic with promising antitumor activity.

Tallysomycin is an antitumor antibiotic complex produced by actinomycetes strain No. E465-94 with antibacterial and antifungal activity. It consists of two major components, A and B.

Jadomycin B is an angucyclic natural product produced by Streptomyces venezuelae ISP5230. It exhibits antimicrobial, antitumor activity and inhibits aurora-B kinase and DNA cleaving. It was also shown to be effective against a variety of staphylococci.

Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity. Marizomib irreversibly binds to and inhibits the 20S catalytic core subunit of the proteasome by covalently modifying its active site threonine residues.

Irofulven is a semisynthetic sesquiterpene derivative of illudin S, a natural toxin isolated from the fungus Omphalotus illudens. Irofulven alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle.

Midostaurin is a multi-target protein kinase inhibitor being investigated for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). It is a semi-synthetic derivative of staurosporine, an alkaloid from the bacterium Streptomyces staurosporeus.

3-(Methylseleno)-L-alanine, a metabolite found in Escherichia coli (strain K12, MG1655), is an inhibitor of DMBA-induced mammary tumors. It has oral bioavailability and can induce cell apoptosis.

Capecitabine inhibits tumor growth and metastatic recurrence after resection of human hepatocellular carcinoma (HCC) in highly metastatic nude mice model. It is a chemotherapy medication used to treat breast cancer, gastric cancer and colorectal cancer.

Palbociclib is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycle arrest.

Lenvatinib is a receptor tyrosine kinase (RTK) inhibitor that has selectivity for VEGFR2. It exhibits antineoplastic activity, and has been indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer.

Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with an IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. Imatinib is an oral chemotherapy agent used to treat cancers. Specifically, it is used for chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL) that are Philadelphia chromosome-positive (Ph+), certain types of gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), systemic mastocytosis, and myelodysplastic syndrome.