derivative

Glyphosate (Atila) is an herbicide. It also is a possible carcinogen to humans.

N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine) is an adenosine derivative and adenosine receptor agonist with Ki values of 11.8 nM for rat A1 receptors and 30.1 nM for human A1 receptors.

MST-312 (Telomerase Inhibitor IX) is a derivative of green tea epigallocatechin gallate (EGCG). MST-312 is a telomerase inhibitor. MST-312 has research value in cancer, such as multiple myeloma (MM).

Carbenoxolone disodium (Duogastrone) salt is an agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise, the drug is low in toxicity.

Hexyl gallate (Gallic acid hexyl ester), an alkyl ester derivative of gallic acid, exhibits potent antimalarial activity against Plasmodium falciparum (IC50: 0.11 mM).

Acipimox (K-9321) is a niacin derivative and nicotinic acid analog with activity as a hypolipidemic agent. Acipimox has special application for the treatment of hyperlipidemia in non-insulin-dependent diabetic patients.

Pivagabine (CXB-722), a hydrophobic 4-aminobutyric acid derivative, exhibits neuromodulatory activity and successfully penetrates the blood-brain barrier in rats. It counteracts the impact of foot shock on GABAA receptor function and corticotropin-releasing factor (CRF) levels in the rat brain.

Acetylspiramycin (Spiramycin B) targets 50S ribosome to inhibit protein synthesis.

Quinoclamine is a naphthoquinone derivative and is an NF-κB inhibitor.

L-Ascorbic acid 2-phosphate magnesium (2-Phospho-L-ascorbic acid magnesium) functions as an antioxidant and stimulates hepatocyte growth factor (HGF) production. This long-acting vitamin C derivative promotes collagen formation and expression.

Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug being developed for delivering nicotinic acid (NIC) into the skin to prevent actinic keratosis and its progression to skin cancer.

L-Ascorbic acid 2-phosphate trisodium (Sodium ascorbyl phosphate) is utilized in biocatalytic dephosphorylation for electric power generation and electrochemical detection assays.

Bz-RS-ISer(3-Ph)-Ome (Methyl (2R,3S)-3-(benzoylamino)-2-hydroxy-3-phenylpropanoate) is a paclitaxel derivative that inhibits the HSV replication cycle at low cytotoxicity, blocks mitosis in Vero cells, affects the size of M-MSV-induced tumors, and influences the immune response by inhibiting PHA-induced proliferation of T lymphocytes.

Dacisteine (N,S-Diacetyl-L-cysteine) is an inhibitor of New Delhi metallo-beta-lactamase-1 (NDM-1) with an IC50 of 1000 μM.

5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT, is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding [1]. [1]. Naiman, N., et al. 2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. Journal of Medicinal Chemistry, 1989; 32(1), 253-256.

MNS is a tyrosine kinases inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.

Tropolone, a metal chelator, possesses weak antioxidative and radical-scavenging properties and shows a strong affinity for ferric ion

Epirubicin hydrochloride (Pharmorubicin) is an adriamycin derivative, a topoisomerase (Topo) inhibitor, and a Forkhead box protein p3 (Foxp3) inhibitor. Epirubicin hydrochloride has antitumor activity.

Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM). Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent.

(-)-Hydroxycitric acid lactone (Garcinia lactone) is an anti-obesity agent and a potent inhibitor of ATP citrate lyase, an enzyme that catalyzes the extramitochondrial cleavage of citrate to oxaloacetate and acetyl-CoA.

Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. Carmofur has been known to induce leukoencephalopathy.

Fudosteine is a novel mucoactive agent and a MUC5AC mucin hypersecretion inhibitor.

Colcemid (NSC-3096) is a microtubule polymerization inhibitor that primarily targets tubulin, with an IC₅₀ of 2.4 μM. Demecolcine interacts with tubulin dimers, induces antimitotic effects, and inhibits microtubule growth. Colcemid is a classic reagent used in karyotyping, banding techniques, and cell cycle synchronization. Colcemid can induce apoptosis and is used in studies of tumor and embryonic cloning.

Antitumor agent-21 (TRX818) is an orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities.