Proxorphan is a N-substituted 6-oxamorphinane patented by American pharmaceutical company Bristol-Myers Co. as opioid analgesic and antitussive drug. Proxorphan acts as a κ-opioid receptor partial agonist and to a lesser extent as a μ-opioid receptor partial agonist.

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.

Mocimycin (also known as kyrromycin) was isolated from Streptomyces ramocissimus and tested in vitro against wide range of bacterias. Although having showed good results, drug did not enter clinical trials. Mocimycin acts by binding tightly and specifically to bacterial EF-Tu. Upon administration the antibiotic prevents EF-Tu-GDP from leaving the ribosome and thus inhibits bacterial protein synthesis. Nowadays, the antibiotic is mainly used to study bacterial protein synthesis at the level of elongation factor EF-Tu-GDP release.

Isoquercetin is a flavonoid, derivative of quercetin. It was isolated from various plant species including Ammothamnus Lehmanii, Caragana alaica, Cicer baldshuanicum, C. macroconthum, C. pungens, Euphorbia cyparissias, E. helioscapia, E. lathyris, E. lucida, E. purporata and others. It demonstrated radical scavenging activity, inhibitory effects on Na+/K+-ATPase and positive inotropic activity. It is protein disulfide isomerase (PDI) inhibitor. As a PDI inhibitor, this agent blocks PDI-mediated platelet activation, and fibrin generation, which prevents thrombus formation after vascular injury. Isoquercetin inhibited the replication of both influenza A and B viruses at the lowest effective concentration. Isoquercetin activates the ERK1/2-Nrf2 pathway and protects against cerebral ischemia-reperfusion injury in vivo and in vitro. It is being investigated for prevention of thromboembolism in selected cancer patients and as an anti-fatigue agent in kidney cancer patients treated with sunitinib.

β-N-Acetyl-D-galactosamine (GalNAc) is an amino sugar derived from galactose found in O-linked and N-linked glycans. As an essential sugar, the role is basically the same for N-acetylgalactosamine as it is for the others, which is to enhance cellular communication. Although there has not been much research to date, what has been done reveals that this saccharide may inhibit the growth of some tumors. For example, colon cancer patients have only half the normal amounts of N-acetylgalactosamine. Studies have shown that colon cancer cells that metastasize make more mucin, making them more likely to form metastases. Therefore, it appears that N-acetylgalactosamine plays an important role in preventing this formation from occurring. N-acetylgalactosamine and N-acetylglucosamine glycans is a predictor of metastasis and poor prognosis in a number of human adenocarcinomas, including breast cancer. Lower than normal levels of this sugar has been found in patients with heart disease implying that these conditions may be reversed if a supplementation of N-acetylgalactosamine were to be added to the diet. It appears that β-N-Acetyl-D-galactosamine plays a role in joint function, sweeping away destructive free radicals that can cause inflammation. N-acetylgalactosamine also seems to play an important role in the immune system. Contained in macrophages and neutrophils, it may play a significant role in the etiology of joint inflammation and could be important in such conditions as rheumatoid arthritis. In humans, it is the terminal carbohydrate forming the antigen of blood group A. N-acetylgalactosamine (GalNAc) is a well-defined liver-targeted moiety benefiting from its high affinity with asialoglycoprotein receptor (ASGPR). By conjugating it directly to the oligonucleotides or decorating it to a certain delivery system as a targeting moiety, GalNAc has achieved compelling successes in the development of nucleic acid therapeutics in recent years. Several oligonucleotide modalities are undergoing pivotal clinical studies, followed by a blooming pipeline in the preclinical stage. N-Acetyl-D-galactosamine is used in affinity chromatography, protein chromatography and in carbohydrate matrices. N-Acetyl-D-galactosamine has been used to study periodontal disease and to facilitate the design of potent small-molecule ice recrystallization inhibitors. N-Acetyl-D-galactosamine has also been used to demonstrate a molecular shuttle between extracellular and cytoplasmic space allows for monitoring of GAG biosynthesis.

Methyl palmoxirate, an oral hypoglycemic agent, was studied as a selective and irreversible inhibitor of the mitochondrial enzyme carnitine palmitoyltransferase and of long-chain fatty acid oxidation to treat diabetes. In addition, this compound was used to study the brain lipid metabolism by quantitative autoradiography or positron emission tomography (PET).