Mideplanin (MDL 62873), a teicoplanin amide derivative, was studied as an antibacterial agent against Gram-positive bacteria. However, further, development appears to have been discontinued.

Arctigenin is a plant lignan extracted from Arctium lappa that has been shown to have estrogenic properties. In ER-positive MCF-7 cells, arctigenin efficiently inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced cell migration and invasion. Arctigenin confers anti-metastatic effects by inhibiting MMP-9 and uPA via the Akt, NF-κB and MAPK signaling pathways on breast cancer, regardless of ER expression. Intake of arctigenin could be an effective supplement for breast cancer patients. Arctigenin is a phenylpropanoid dibenzylbutyrolactone lignan compound possessing antitumor, anti-inflammatory, anti-influenza, antioxidant, antibacterial, and hypoglycaemic activities. Arctigenin exhibited significant antiproliferative activity against CCRF-CEM cells after 72 h treatment with IC50 values of 1.21 ± 0.15 um. It arrested CCRF-CEM cells in the S phase. It induced apoptosis in CCRF-CEM cells in a concentration- and time-dependent manner. Arctigenin is a good candidate for the development of novel agents against T-cell lymphoma. Arctigenin has been found to act as an agonist of adiponectin receptor 1 (AdipoR1). Arctigenin is an antagonist of MR and effectively decreases the Na/K-ATPase 1 gene expression, thus highlighting its potential as an anti-hypertensive drug lead compound.

Profadol is a pyrrolidine derivative patented in the 1960s by pharmaceutical company Parke-Davis as opioid analgesic. Profadol acts as a mixed agonist-antagonist of the μ-opioid receptor and in preclinical studies, Profadol precipitates abstinence in morphine-dependent monkeys and can reverse pethidine- induced narcosis in nondependent monkeys. In morphine-dependent human subjects, Profadol was also found to pre¬cipitate acute abstinence syndromes, with a potency 40 to 50 times less than that of nalorphine. Profadol, unlike other morphine-antagonists, does not produce nalorphine-like subjective effects. Over a fourfold range of doses, this drug was found to produce subjective effects indistinguishable from those of morphine. Also unlike other morphine-antagonists, profadol is quite active on the "classical" rodent tests for analgesia. It is about 1.3 times as potent as pethidine on the mouse hot-plate test, and about four times as potent on the rat tail-pressure test.

Ilmofosine (1-hexadecylthio; 2-methoxyethyl-racglycero-3-phosphocholine) is a synthetic 1-S-thioether alkyl lysophospholipid derivative with potential antineoplastic activity. In extensive preclinical evaluation against tumor cell lines and in the human tumor colony-forming assay, Ilmofosine was cytotoxic against both leukemias and solid tumors. Ilmofosine was effective against many tumor types, including ovary, non-small cell lung, kidney, and melanoma. Ilmofosine exhibited competitive inhibition of protein kinase C activity with respect to phosphatidyl-serine and inhibited the enzyme activated by diolein.

Veribulin is a novel microtubule destabilizer that both functions as a potent cytotoxin and acts as a vascular disrupting agent (VDA). It binds to the same (or nearby) sites on β-tubulin as colchicine. It is capable of evading multidrug resistance pumps and, thus, achieves high CNS concentrations. It is efficacious in multiple xenograft models without CNS toxicity. Veribulin had previously demonstrated pre-clinical and clinical activity in multiple tumor types. Veribulin is in phase II clinical trial for the treatment of Glioblastoma and Malignant melanoma.

Triciribine is a purine analogue which inhibits DNA and protein synthesis, it is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt1. In whole cells triciribine is phosphorylated by adenosine kinase which may be necessary for its activity. Triciribine is a cancer drug which was first synthesised in the 1970s and trialled clinically in the 1980s and 1990s without success. Following the discovery in the early 2000s that the drug would be effective against tumours with hyperactivated Akt, it is now again under consideration in a variety of cancers. As PTX-200, the drug is currently in two early stage clinical trials in breast cancer and ovarian cancer being conducted by the small molecule drug development company Prescient Therapeutics.

Cethexonium is a cyclohexanols derivative with antimicrobial activities.

Tubulozole is a stereospecific microtubule inhibitor. Structurally it is related to the benzimidazole carbamates by its carbamate moiety, which is essential for the activity of both types of compounds. The compound exists as a cis-isomer called tubulozole-C (R 46 846) and as a trans-isomer called tubulozole-T. The cis-isomer appears to be a potent and specific microtubule inhibitor, the trans-isomer being inactive at 100 times higher concentrations. At low concentrations, both isomers of tubulozole (C, T) inhibit Plasmodium falciparum but only tubulozole C inhibits mammalian cells. Since tubulozole C prevents polymerization of mammalian tubulin whereas tubulozole T does not, the antimalarial action of tubulozoles may not involve microtubules. Tubulozole-C, a new synthetic anticancer drug, interfered with the structure and function of microtubules in both interphase and mitotic cells. The activity of Tubulozole-C in experimental tumor systems can be explained partly by a direct antimitotic effect and partly by the disintegration of the normal subcellular organization of the nondividing cells. At concentrations which affect the microtubule system, tubulozole-C arrested directional migration of transformed cells and malignant invasion in a three-dimensional organ culture system. Investigations in vivo show that malignant L1210 leukemia cells are more susceptible to the antimicrotubular effect of tubulozole-C than are the normal leukocytes of the host. The trans-isomer of tubulozole (tubulozole-T, R 48 265), which has no antitumor activity in vivo, did not affect the microtubule system of cells in vitro or their capacity for directional migration or for malignant invasion.

Semapimod (CNI-1493) is a cytokine inhibitor and synthetic guanylhydrazone mitogen-activated protein kinase blocker, is being developed by Cytokine PharmaSciences as a potential treatment for Crohn's disease and other inflammatory conditions. As of December 2001, a phase I study demonstrating the safety of the compound had been completed and phase II trials for psoriasis and Crohn's disease were ongoing. In April 2003, preclinical and early clinical studies were underway for a variety of indications, including congestive heart failure and pancreatitis. Semapimod inhibits activation of p38 MAPK and NF-κB and induction of cyclooxygenase-2 by TLR ligands, but not by IL-1β or stresses. Semapimod inhibits TLR4 signaling (IC50 ≈0.3 umol) and acts by desensitizing cells to LPS; it fails to block responses to LPS concentrations of ≥5 ug/ml. Semapimod had been in phase II clinical trials by Ferring Pharmaceuticals for the treatment of Crohn's disease. However, this research has been discontinued. Semapimod is in phase I clinical trials for the treatment of autoimmune disorders and inflammation.