Chlorsulfaquinoxaline is a halogenated derivative of sulfaquixonaline, an immunosuppressive and antifungal agent used in the control of coccidiosis in poultry, rabbit, sheep, and cattle. In vitro, Chlorsulfaquinoxaline acts as a topoisomerases IIα and IIβ poison, thus inhibiting DNA replication. Chlorsulfaquinoxaline shows good activity against human tumor cells in the human tumor colony-forming assay and subsequently has shown activity against murine and human solid tumors. No major objective antitumor responses was observed during Chlorsulfaquinoxaline Phase II clinical evaluation in non-small-cell lung cancer and metastatic colorectal cancer. Chlorsulfaquinoxaline was well tolerated with hypoglycemia being the most clinically significant toxicity.

Mitindomide was studied as an antineoplastic agent that inhibited the activity of the topoisomerase II. The drug underwent preclinical development; however, this study was discontinued.

Embusartan or BAY106734 (6-n-butyl-4-methoxycarbonyl-2-oxo-1[(2'-(1H-tetrazol-5-yl) -3-fluorobiphenyl-4-yl)methyl] 1,2-dihydropyridine) is an angiotensin II receptors antagonist. Embusartan has beneficial effects in different animal hypertension models. Embusartan appears as a potent and specific new inhibitor of angiotensin II-induced growth-related events in vascular smooth muscle cells. It was being developed for the treatment of hypertension.

Elsamitrucin is a heterocyclic antineoplastic antibiotic isolated from the bacterium Actinomycete strain J907-21. Elsamitrucin intercalates into DNA at guanine-cytosine (G-C)-rich sequences and inhibits topoisomerase I and II, resulting in single-strand breaks and inhibition of DNA replication. It demonstrated a broad spectrum of in vitro cytotoxicity against tumor cell lines. According to the results of Phase II trials elsamitrucin is not an active drug in patients with metastatic breast cancer, colorectal cancer, non-small cell lung cancer or ovarian cancer, however, it showed modest activity in patients with relapsed or refractory non-Hodgkin's lymphoma.

Elisartan (HN 65021) is a selective, orally active, nonpeptide angiotensin II (AT1) antagonist. It antagonizes angiotensin receptor-mediated vasoconstriction. Elisartan was being assessed for the treatment of hypertension.

Ripisartan (UP-269-6) is a specific nonpeptide angiotensin II receptor antagonist. Oral administration of ripisartan in rats and dogs resulted in a dose-dependent and long-lasting inhibition of the angiotensin II-induced pressor response. It did not show agonistic properties in animals. In vitro, ripisartan was found to bind selectively to AT1 receptors. In humans, it showed high biliary excretion and reabsorption. Canine studies have suggested it might have cardioprotective properties after acute ischemia-reperfusion.

Phenethyl isothiocyanate (PEITC) presents in cruciferous vegetables which have been shown to decrease the risk of various types of malignancies. PEITC targets multiple proteins to suppress various cancer-promoting mechanisms such as cell proliferation, progression and metastasis. PEITC induces apoptosis in human colon cancer HT-29 cells, prostate cancer cells, and osteogenic sarcoma U-2 OS cells. Unique to prostate cancer is that PEITC downregulates the transcriptional factor Sp1, a regulator of AR expression. PEITC suppresses 4-(methylnitrosamino)-1-(3-pyridyl)-1-butoneinduced pulmonary neoplasia in A/J mouse lung, exhibits cancer chemopreventive activity in rat and reduces azoxymethane-induced colonic aberrant crypt foci formation. PEITC appears to be a promising agent for cancer therapy and is already under clinical trials for leukemia and lung cancer.

Idronoxil (Phenoxodiol) is a synthetic flavonoid derivative developed by MEI Pharma for cancer treatment. Idronoxil inhibits proliferation of many cancer cell lines and induces apoptosis by disrupting FLICE-inhibitory protein, FLIP, expression and by caspase-dependent and -independent degradation of the X-linked inhibitor of apoptosis, XIAP. In addition, Idronoxil sensitizes drug-resistant tumour cells to anticancer drugs including paclitaxel, carboplatin, and gemcitabine. The antiproliferative effects of Idronoxil are associated with inhibition of plasma membrane electron transport in tumour cell lines and primary immune cells. Idronoxil displays anti-cancer activity against all forms of cancer tested in vitro and in vivo to date, using cells representative of all major forms of cancer. While having a modest ability to kill cancer cells(IC50 range between about 1-5 uM), preclinical studies point to its optimal use being to sensitize cancer cells to the toxic effects of standard therapies (chemotherapy and radiotherapy). The rationale is that a sub-lethal inhibitory effect on sphingosine kinase activity reduces the ability of the cancer cell to operate drug-resistance mechanisms and to effect repair of drug- or radiation-induced damage to DNA. In the case of cytotoxic drugs such as cisplatin, carboplatin, paclitaxel, Doxorubicin, and gemcitabine, Idronoxil is an exquisite sensitizer, increasing the cytotoxic potential of those agents by between 103 -105 times, in the process restoring sensitivity to cancer cells highly refractory to those agents.

Picropodophyllin (also known as picropodophyllotoxin (PPP)), an orally active insulin-like growth factor 1 receptor (IGF1R) inhibitor that exhibits no activity at the insulin receptor, FGFR, PDGFR or EGFR. Picropodophyllin possesses antineoplastic activity. PPP is currently tested as an orally administrated single agent treatment in an open-label combined Phase I/II clinical study in advanced cancer patients with solid tumors which progress in spite of several lines of treatment. In addition, it effectively inhibits rhambodmyosarcomas tumor proliferation and metastasis in vitro and in an animal model.

Amonafide is an imide derivative of naphthalic acid. It is a novel topoisomerase II (Topo II) inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA. Amonafide retains cytotoxic activity even in the presence of P-glycoprotein (Pgp)-mediated multi-drug resistance (MDR). It is a new investigational anticancer drug. Amonafide has been extensively studied in patients with malignant solid tumors, like prostate cancer, breast cancer and others. When its usefulness in the treatment of various solid malignancies proved limited, focus was shifted to establishing its use as an antileukemic agent, specifically against secondary and treatment-associated acute myeloid leukemia (AML).