Antineoplastic

14-O-Acetylindolactam V is an antibiotic isolated from the Actinomyces NA34-17. 14-O-Acetylindolactam V has the effect of inducing early Epstein-Barr virus antigen.

Acetomycin is an anti-human tuberculosis and amoeba antibiotic isolated from the Streptomyces ramnlosus. Acetomycin is an anti-biotic, anti-fungal, anti-protozoal, and anti-bacterial agent.

Chromomycin A3 is produced by the strain of Streptomyces olivochromogenes 69895. The major component of the chromomycin complex of the aureolic acid class; isolated from several streptomyces species; exhibits a broad biological profile as an antibacterial, antifungal and antitumour agent; binds reversibly to GC-specific DNA ligand in the minor groove which inhibits transcription, DNA gyrase and topoisomerase II activity.

It is produced by the strain of Streptomyces refuineus var. thermotolerans. It has a weak activity against gram-negative bacteria, and has the effect of inhibiting metamorphoses, vaginal trichomonas and rat tube nematode. It has inhibitory effect on sarcoma 180, L-1210, CA-755, Ascitic ascites type and solid type cancer.

It is produced by the strain of Actinomadura carminata. Intravenous injection of 2 to 4 times of yangerythromycin (1.3-2.25mg) in mice could inhibit the growth of bronchial carcinoma, transplanted gastric cancer, lymphoid leukemia L-1210 and lymphosarcoma, but had poor effect on sarcoma-180 and lymphangiopathy, and had no effect on Eilinite ascites carcinoma.

Epothilons B is a 16-membered macrolide antibiotic produced by the myxobacterium Sorangium cellulosum, which is used as a microtubule stabilization agent (EC0.01 = 1.8 μM). It has strong cytotoxicity and has the effect of resisting plant pathogenic fungi.

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

Dihydrocarminomycin is an anthracycline antibiotic that can be produced by Streptomyces atroviolaceus DS 8938, Str. coeruleorubidus DS 8899, DS 31723, DS 7126 and Str. bifurcus DS 23219.

Illudin S is a natural sesquiterpene agent with strong anti-tumour activity. Illudin S inhibits DNA synthesis via an unknown mechanism.

Mitomycin C is a quinone mitomycin antibiotic produced by Str. caespitosus NRRL 2564. It has antibacterial, antimycobacterial and antiviral activities. And it has an inhibitory effect on tumors.

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

Epirubicin EP Impurity F is an impurity of Epirubicin, which is an anthracycline topoisomerase inhibitor used as an antineoplastic agent.

Staurosporine, also known as antibiotic AM-2282 or STS, is a broad spectrum protein kinase inhibitor produced by Streptomyces sp. Enzymes inhibited include protein kinase C (IC50 = 3 nM), protein kinase A (IC50 = 7 nM), p60v-src tyrosine protein kinase (IC50 = 6 nM) and CaM kinase II (IC50 = 20 nM). Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive.

Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM and 790 nM, respectively.

The citrate salt form of Ixazomib which is a proteasome inhibitor. It is undergoing a rollover Phase II trial against multiple myeloma, amyloidosis and lymphoma in sorts of countries. IC50 = 3.4 nM.

Fumagillin is a compound isolated from the fungus Aspergillus fumigatus. Fumagillin is an antimicrobial agent used in the treatment of microsporidiosis. Fumagillin shows promise as both an anti-infective and antiangiogenic agent.

Oligomycin A, an ATP synthase inhibitor and a macrolide antibiotic with fungicidal activity isolated from Streptomyces species, inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria.

It is produced by the strain of Streptomyces griseolus. It inhibits protein synthesis. it has anti-fungal, anti-fine bacteria, anti-tumor and antigenic insect action.

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.

Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling. Regorafenib is demonstrated to increase the overall survival of patients with metastatic colorectal cancer and has been approved by the US FDA on September 27, 2012.