A novel active metabolite of the anti-cancer drug Tamoxifen. It showed potent ER binding property, blocked estrogen stimulated growth of breast cancer cell and half maximal inhibition of estrogen responsive gene expression in ER pos. human breast cancer cell line. Endoxifen E-isomer is the E-isomer of (Z)-Endoxifen. (Z)-Endoxifen, an active metabolite generated via actions of CYP3A4/5 and CYP2D6, is a more potent selective estrogen receptor modulator (SERM) than Tamoxifen. InVitro: Endoxifen exists as the potently anti-estrogenic (Z)-isomer and the lesser known (E)-isomer. It is assumed that (E)-Endoxifen, structurally related to (E)-4-OH-tamoxifen, have similar pharmacological properties. The (E)-isomer is an impurity in (Z)-Endoxifen drug substance and increases under certain storage conditions. (E)-Endoxifen is identified as the primary degradant.
Endoxifen E-isomer hydrochloride is a potent anti-estrogen drug that is used in the treatment of breast cancer. It is a metabolite of tamoxifen, which is a widely used drug for the treatment of breast cancer. Endoxifen E-isomer hydrochloride has been found to be more effective than tamoxifen in inhibiting the growth of breast cancer cells.
Telotristat is a small molecule drug that is used to treat carcinoid syndrome, a rare condition that occurs in patients with neuroendocrine tumors. It works by inhibiting the production of serotonin, a hormone that is overproduced in patients with carcinoid syndrome. This paper will discuss the method of synthesis or extraction of telotristat, its chemical structure and biological activity, its biological effects, applications in medical, environmental, and industrial research, and future perspectives and challenges.
Bisoctrizole is a chemical compound that belongs to the class of benzotriazole derivatives. It is widely used in various fields, including medical, environmental, and industrial research. Bisoctrizole is known for its excellent UV-absorbing properties, making it a popular ingredient in sunscreens and other cosmetic products.
AZ 505 is an inhibitor of the lysine N-methyltransferase SMYD2 (IC50 = 0.12 μM). It is selective for SMYD2 over SMYD3, DOT1L, EZH2, GLP, G9A, and SET7/9 (IC50s = >83.3 μM). AZ 505 (10 mg/kg) delays cyst growth in early- and late-stage Pdk1 conditional knockout mouse models of polycystic kidney disease. AZ505 is a potent and highly selective inhibitor of SMYD2 with potential anticancer activity. AZ505 is composed of three distinct moieties: benzooxazinone, cyclohexyl, and dichlorophenethyl substituents. The structure of the ternary complex reveals that a single AZ505 molecule is bound in the peptide binding groove of SMYD2.
4'-(3-((3R)-3-(Dimethylamino)pyrrolidinyl)propoxy)(1,1'-biphenyl)-4-carbonitrile, also known as DPCPX, is a potent and selective antagonist of the adenosine A1 receptor. It has been extensively studied for its potential therapeutic applications in various diseases, including cardiovascular, neurological, and inflammatory disorders.
KX2-391 dihydrochloride is a small molecule inhibitor that has shown promising results in preclinical studies for the treatment of various cancers, including melanoma, prostate, and breast cancer. It is a derivative of the Src kinase inhibitor, PP1, and has been shown to inhibit the activity of Focal Adhesion Kinase (FAK), a protein that plays a crucial role in cell migration, invasion, and survival.
Imazapic is a herbicide that is widely used in agriculture to control weeds. It belongs to the imidazolinone family of herbicides and is known for its broad-spectrum activity against a wide range of weeds. Imazapic is also used in medical and environmental research due to its unique chemical structure and biological activity.
4-(2-Aminopropyl)phenol, also known as 4-AP-3-OH or p-AP-3-OH, is a chemical compound that belongs to the family of phenols. It is a derivative of phenethylamine and has a molecular formula of C9H13NO. This compound has been studied for its potential therapeutic and toxic effects, as well as its role in environmental pollution management and industrial manufacturing processes.