Lavendustin B is a weak tyrosine kinase inhibitor that has been used as a negative control for lavendustin A. Lavendustin A strongly inhibits epidermal growth factor receptor-associated tyrosine kinase, competes with ATP, and is noncompetitive with the peptide. Lavendustin B was previously identified as an inhibitor of HIV-1 integrase (IN) interaction with its cognate cellular cofactor, lens epithelium-derived growth factor (LEDGF/p75).

Lavendustin C or HDBA (2-hyroxyl-5-(2,5-dihydroxybenzylamino) benzoic acid) is the active pharmacophore of lavendustin A, a tyrosine kinase inhibitor isolated from a butyl acetate extract of Streptomyces griseolavendus.

Bufalin is a traditional oriental medicines, originally isolated from the Chinese toad venom. Bufalin is a cardiotonic steroid that has the potential to induce differentiation and apoptosis of tumor cells. Research on bufalin has so far mainly involved leukemia, prostate cancer, gastric cancer and liver cancer, and has been confined to in vitro studies. The bufadienolides bufalin and cinobufagin have been shown to induce apoptosis in a wide spectrum of cancer cell. Bufalin has being shown to be a potent small-molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1. Bufalin is a component of Huachansu, a Chinese medicine that comes from dried toad venom from the skin glands of Bufo bufo gargarizans Cantor or B.melanotictus Schneider, has been used in the treatment of various cancers in China.

Piceatannol (3,3′,4,5′-tetrahydroxy-trans-stilbene; PIC) is a naturally occurring stilbene present in diverse plant sources. Piceatannol is a hydroxylated analog of resveratrol and produced from resveratrol by microsomal cytochrome P450 1A11/2 and 1B1 activities. Like resveratrol, Piceatannol has a broad spectrum of health beneficial effects, many of which are attributable to its antioxidative and anti-inflammatory activities. Piceatannol exerts anticarcinogenic effects by targeting specific proteins involved in regulating cancer cell proliferation, survival/death, invasion, metastasis, angiogenesis, etc. in the tumor microenvironment. Piceatannol also has other health promoting and disease preventing functions, such as anti-obese, antidiabetic, neuroprotective, cardioprotective, anti-allergic, anti-aging properties. A comprehensive review of PIC concludes that the compound has the health promoting and disease preventive potential. However, low water-solubility and bioavailability of PIC limit its pharmaceutical application and also use in functional foods. In this context, it is noticeable that beta-cyclodextrin was found to improve the bioavailability, the solubility and the stability of Piceatannol.

Tyrphostin A23 belongs to a novel class of low molecular weight proteins that inhibit protein tyrosine kinase and block the EGF-dependent autophosphorylation of the receptor. It has been considered as potential anti-cancer drug. It inhibits pancreatic cancer cell growth in vitro. Inhibition of EGF receptor by tyrphostin A23 was associated with a significantly increased proportion of apoptotic cells in human prostate cancer DU145 cell culture.

Thiolutin is a naturally occurring bicyclic dithiole that was first isolated from Streptomyces luteorectiuli based on its antibiotic activities. Thiolutin inhibits the growth of Saccharomyces cerevisiae and several gram-positive and -negative bacteria by inhibiting DNA-dependent RNA polymerases. It also inhibits the adhesion of endothelial cells, including adhesion of human umbilical vein endothelial cells (HUVECs) to vitronectin, and restricts tumor cell-induced angiogenesis.

AG1478 (also known as Tyrphostin AG 1478 ) is a selective EGFR inhibitor, which induced cell cycle arrest in G1 phase, is developed as potential drug for nasopharyngeal carcinoma treatment. In addition was shown, that AG1478 effectively blocked the leiomyoma cell growth and is unaffected by the presence of physiological concentrations of progesterone and estradiol. The growth-arresting properties of AG1478, unaffected by ovarian steroidal hormones, identify it as a potential lead agent for the non-surgical management of uterine leiomyomas. Also was investigated the action of the combination AG1478 in combination with HGF tyrosine kinase inhibitors on non-small cell lung cancer (NSCLC) cells, and was suggested, that these combinations of drugs could be potentially used for treatment of NSCLC.