Gambogic acid (GA), a naturally occurring xanthone-based moiety, reported from Garcinia hanburyi tree, is known to perform numerous intracellular and extracellular actions, including programmed cell death, autophagy, cell cycle arrest, antiangiogenesis, antimetastatic, and anti-inflammatory activities. In addition, GA-based synergistic approaches have been proven to enhance the healing strength of existing chemotherapeutic agents along with lesser side effects. Among cellular targets of gambogic acid topoisomerase, multidrug-resistant protein ATP-binding cassette transporter B1 (ABCB1) and Transferrin receptor.

Corydine is a naturally occurring compound which can be extracted from plants such as Chelidonium majus, Corydalis marschalliana, C. bulbosa, C slivenensis, Glaucium grandiflorum. Corydine has shown some efficacy as an anti-cancer compound in several cell models and was examined along with related compounds from Stephania dinklagei for antiprotozoal activities. (+)- and (-)- Corydine were tested as neuromuscular blocking agents were it was found that there was a modest preference for (+)-corydine.

O-Methyl-Gambogic acid Methyl Ester (aka dimethyl-Gambogic acid) is a derivative of gambogic acid a naturally occurring compound found in the resin excreted by the garcinia hanburryi tree in Southeastern Asia. Dimethyl-Gambogic acid demonstrates antiapoptotic activity in T17 cells with an EC50 of 120 nM. It has also shown efficacy against the parasite Trypanosoma brucei with an IC50 of 1.3 micro-M.

Shikonin is a major naphthoquinone compound found in the roots of Lithospermum erythrorhizon and exhibits powerful anticancer activities for various cancer cells. Shikonin and its derivatives are characterized by a wide spectrum of antibacterial activities: high antibacterial activity towards Gram-positive bacteria (Staphylococcus aureus et al.), a stable fungicidal effect towards Candida and Trichosporon fungi. Shikonin normalizes the production of the key mediators of inflammation IL-1 and IL-2, IFN-γ, reduces vascular permeability in the focus of inflammation, exhibiting a marked anti-inflammatory effect. Combined therapy with applications of a bio-polymeric film with shikonin and its esters (naphthoquinone derivatives) led to an obvious improvement of the clinical parameters and reduced the morphological signs of the buccal mucosal lesions. The drug was well tolerated by all patients and no side effects were recorded. Shikonin, as a naturally occurring, low-molecular-weight pan-chemokine receptor inhibitor, constitutes a basis for the development of novel anti-HIV therapeutic agents.

Gallein is an inhibitor of G protein beta gamma subunit signaling. It exerts antineoplastic action in vitro and anti-inflammatory action in vivo. Gallein may be used in histological staining.

The bioactive quinone Alpha-lapachone was originally isolated from the heartwood of trees of the Bignoniaceae family (Tabebuia sp). It can also be found in other families such as Verbenaceae, Proteaceae, Leguminosae, Sapotaceae, Scrophulariaceae, and Malvaceae. Alpha-Lapachone showed potent cytotoxicity against different cancer cell lines. Alpha-lapachone is an "irreversible" inhibitor of topoisomerase II. Alpha-lapachone demonstrated antibacterial activity against pathogenic organisms Staphylococcus aureus and Salmonella typhi and antifungal activity against Candida albicans and Trichophyton mentagrophytes.

K-858 is a small molecule inhibitor of Eg5 (kinesin spindle protein), a mitotic kinesin that plays an essential role in establishing mitotic spindle bipolarity. K-858 blocked centrosome separation, activated the spindle checkpoint, and induced mitotic arrest in cells accompanied by the formation of monopolar spindles. K858 induces mitotic arrest, apoptosis, and cell growth inhibition in cancer cells. K-858 exhibited potent antitumor activity in xenograft models of cancer, and induced the accumulation of mitotic cells with monopolar spindles in tumor tissues.

BX-517 is a nanomolar inhibitor of phosphoinositide-dependent kinase-1 (PDK-1), developed by Berlex Biosciences. BX-517 blocked activation of Akt in tumor cells. The compound was not developed further due to solubility an bioavailability issues.

AZ-628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays. Specificity profliling indicates that AZ-628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ-628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation. The profile of AZ-628 cross-reactivity suggests that similar to sorafenib, AZ-628 may be antiangiogenic based on inhibition of VEGFR2. AZ-628 is remarkably effective at inhibiting the growth of a specific subset of human cancer cell lines derived from melanomas, thyroid cancers, and colorectal cancers that harbor the BRAF V600E mutation. Preclinical evaluation is in progress.

AZD-5597 is potent imidazole pyrimidine amide CDK inhibitor with in vitro anti-proliferative effects against a range of cancer cell lines. AZD-5597 exhibited excellent aqueous solubility, photostability, hydrolytic stability, plasma stability and the lack of CYP inhibition. In nude mice implanted subcutaneously with SW620 human colon adenocarcinoma cells, AZD-5597 (15 mg/kg, dosed intermittently for 3 weeks, ip) inhibited tumor volume by 55%. The overall profile of AZD-5597 indicated that it was suitable for further development as an iv agent.