Antineoplastic

Safracin B is a new antibiotic from the family of Safracin produced by Pseudomonas fluorescens A2-2. Safracin B exhibits broad spectrum antimicrobial and strong antitumor activities.

Mimosamycin is a glycoside antibiotic produced by Str. argillaceus, Str. plicatus and Str. tanashiensis. It has anti-Gram-positive bacteria and mycobacterial activity. It can inhibit HeLa cells.

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.

Porfiromycin is a quinone antibiotic produced by Str. ardus NRRL 2817. It has anti-Gram-positive and negative bacteria activity. It can inhibit sarcoma-180, Ehrlich ascites carcinoma, L-1210, H leukemia (solid type). The dose of inhibiting KB cell protein synthesis is 0.5 μg/mL. It is a bioreductive DNA alkylating agent that preferentially kills hypoxic tumor cells relative to other aerobic counterparts.

Netropsin is isolated from Streptomyces netropsis as a basic polypeptide. It can specific bind to A-T areas of DNA that is very useful to genetic research. Netropsin can disrupt the cell cycle, prolonging G and arresting in G. Netropsin has antibiotic and antiviral activity. It has been shown that Netropsin is active against Gram-positive and Gram-negative bacteria.

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 Str. pactum var. pactum NRRL 2939. It is a cyclopentane and cyclohexane derivative antibiotic. It has anti-bacterial, virus, tumor activity.

It is produced by the strain of Streptoverticillium verticillum 843-1. It's a heteropeptide antibiotic. It has anti-gram-positive bacteria, negative bacteria and mycobacterium effects. The therapeutic index of the complex for Solid Adenocarcinoma and Sarcoma-180 are 16. The therapeutic index of Ehrlician ascites cancer is 4-8. It acts an antibiotic originally, an anticancer agent and a selection agent for transformed algae, protista, animal and fungal cells.

A hydrophobic cyclodepsipeptide with potent antitumour activity; a highly selective potassium ionophore; a biosensor to detect potassium efflux.

Streptozotocin is a monosaccharide antibiotic produced by Str. achromogenes 128 (NRRL 2697). It has antibacterial effect, and human serum and urine do not affect its activity. It can protect mice infected with Staphylococcus aureus, Pasteurella pestis and Proteus vulgaris. The same amount of antibiotic U-15774 can inhibit mouse sarcoma-180, sarcoma L5178Y, Walker-256 and Ehrlich carcinoma. Streptozotocin is a glucosamine-nitrosourea derivative, which is a DNA-methylating, carcinogenic, antibiotic and diabetes inducing agent. It is commonly used for the treatment of metastatic pancreatic islet cell carcinoma.

Tallysomycin A is a glycopeptide antibiotic produced by the rare actinomycete No. E 465-94. It has anti-gram-positive bacteria and gram-negative bacteria and fungi activity. It can induce lysogenic E. coli W1709 (A) to release phage.

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.

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.

Bleomycin A5 hydrochloride is an antitumor antibiotic which induces apoptosis.

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.

Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.

Paclitaxel is a compound with anti-tumor activity extracted from the Pacific yew tree Taxus brevifolia. Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.

Pentostatin is an adenosine deaminase inhibitor isolated from Streptomyces and effective against cancer cell lines. Pentostatin is a purine nucleoside analog that irreversibly inhibits adenosine deaminase (Ki = 0.9 pM) and thus interrupts DNA synthesis in dividing cells. Pentostatin has been reported to display strong efficacy in the clinical treatment of hairy cell leukemia as well as relapsed chronic lymphocytic leukemia.

An unusual anthracycline produced by streptomyces nogalater var. Nogalater. It is a potent antibacterial and antitumor agent that interacts with DNA by intercalation.

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.