Sinefungin, a natural nucleoside isolated from cultures of Streptomyces incarnatus and S. griseolus, is structurally related to S-adenosylhomocysteine and S-adenosylmethionine. Sinefungin is a DNA methyltransferase (DNMT) inhibitor (IC₅₀ = 0.1 - 20 uM). Sinefungin has been shown to inhibit the development of various fungi and viruses, but its major attraction to date resides in its potent antiparasitic activity. This compound has been reported to display antiparasitic activity against malarial, trypanosomal, and leishmanial species. Sinefungin inhibits pneumococcal biofilm growth in vitro and colonization in vivo, decreases AI-2 production, and downregulates luxS, pfs, and speE gene expressions. Sinefungin was significantly suppressive against both L. donovani and L. braziliensis panamensis infections in hamsters when compared with meglumine antimonate. An immunosuppressed rat model was used to investigate the anti-Cryptosporidium parvum activity of sinefungin. In infected animals, oral sinefungin therapy resulted in a dose-related suppression of oocyst shedding, which correlated with oocyst disappearance from ileal sections. When administered prior to or on the day of oocyst challenge, sinefungin successfully prevented infection. These data suggest that sinefungin could be considered as a candidate molecule in the treatment of human cryptosporidiosis, considered to be the most significant enteric opportunistic infection in AIDS.

Satranidazole is a drug that helps to combat a large number of varied health disorders effectively. This drug participated in clinical trials in patients of amebic liver abscess, where it showed a far lower incidence of side effects and had a significantly better tolerance than metronidazole. Besides, satranidazole has been studied an adjunct to scaling and root planning in the treatment of chronic periodontitis. satranidazole has a low polar surface area, high dose, and dosing frequency. Nanosizing with appropriate stabilizers and programmed processing conditions successfully produced SAT-NC with improved pharmaceutic and pharmacokinetic characteristics.

2-Cyano-3,12-dioxooleana-1,9-diene-28-oic acid (CDDO, also known as Bardoxolone) is a synthetic triterpenoid that displays potent anti-inflammatory and antitumorigenic activities. CDDO was in the clinical trial phase I for the treatment patients with Solid tumors and leukemia, but that studies were discontinued. It is known, that CDDO blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2. In addition, was discovered, that CDDO disrupted intracellular redox balance and thereby induce apoptosis. Moreover, CDDO is a ligand for peroxisome proliferator-activated receptor that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.

Litronesib is a specific, ATP-uncompetitive, allosteric, and potent small-molecule inhibitor of Eg5 with potential antineoplastic activity. Litronesib selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and consequently cell death in tumor cells that are actively dividing. Histone-H3 phosphorylation of tumor and proliferating skin cells is a promising pharmacodynamic biomarker for in vivo anticancer activity of litronesib. Litronesib had been in phase I clinical trial for the treatment of solid tumors. The most frequent-related adverse events were hematologic such as neutropenia.

M40419 (now GC4419) is a Mn(II)-containing pentaazamacrocyclic selective superoxide dismutase mimetic. It is a first-in-class, small molecule enzyme mimetic that converts superoxide to hydrogen peroxide and molecular oxygen. GC4419 is currently being evaluated in an ongoing randomized Phase 2 clinical trial to assess its effect on the incidence, severity and duration of severe oral mucositis (OM) when given to patients with squamous cell cancers of the head and neck in combination with radiation and chemotherapy. GC4419 has received Breakthrough Therapy and Fast Track designations from the U.S. Food and Drug Administration.

Dinaline represents a group of pharmacologically active lipophilic substances with a relatively simple structure derived from N-acyl-o-phenylenediamine. It has been found to exhibit high antineoplastic activity in a series of slowly growing tumors such as chemically induced rat mammary and colorectal carcinomas, osteosarcoma C22LR and Brown Norway myeloid leukemia. The drug was inactive against many of the typically hypersensitive signal tumors, i.e. mouse leukemias P388 and L1210, sarcoma 180 and Yoshida sarcoma. Colon carcinoma cells exposed to dinaline demonstrate distinct but reversible changes in amino acid transport, protein metabolism, DNA synthesis and cell proliferation.

ABT-102 is a selective antagonist of transient receptor potential vanilloid type 1 (TRPV1), designed for the treatment of nociceptive pain. ABT-102 potently blocks multiple modes of TRPV1 receptor activation and effectively attenuates downstream consequences of receptor activity.