Miconazole is a broad-spectrum azole antifungal with some activity against Gram-positive bacteria as well. It is widely used to treat mucosal yeast infections, including both oral and vaginal infections; although intravenous miconazole is no longer available, a wide variety of suppositories, creams, gels, and tablet-based products are available. Miconazole is thought to act primarily through the inhibition of fungal CYP450 14α-lanosterol demethylase activity. Miconazole was first synthesized in 1969 and first granted FDA approval on January 8, 1974, for sale by INSIGHT Pharmaceuticals as a topical cream. It is currently available as a variety of prescription and over the counter products. Despite having been in clinical use for an extended period, resistance to miconazole among susceptible organisms is relatively low.
Trans-methylferulate is a cinnamate ester that is the methyl ester of ferulic acid. It has been isolated from Pisonia aculeata. It has a role as a plant metabolite. It is a cinnamate ester, a methyl ester and a member of guaiacols. It is functionally related to a trans-ferulic acid.
Frequency of aberration-bearing cells induced by the monolignol methyl ferulate 6 and its catechol derivative methyl caffeate 9 in V79 cells in vitro.
Lapatinib is an organofluorine compound, an organochlorine compound, a member of quinazolines and a member of furans. It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It is functionally related to a monofluorobenzene.
Structures of some approved and reported ErbB family inhibitors: Lapatinib, TAK-285
The alignment between the bioactive conformer of lapatinib (I) (colored in violet) and the docked pose (colored in green) at EGFR binding site.
Left: Docking of lapatinib (I) in EGFR binding site (PDB code: 1XKK) showing H bonds with met793 and π interaction with Lys 745. Right: Docking of (TAK285) (III) in HER-2 binding site (PDB code: 3RCD) showing H bond with met801.
Doxorubicin is a deoxy hexoside, an anthracycline, an anthracycline antibiotic, an aminoglycoside, a member of tetracenequinones, a member of p-quinones, a primary alpha-hydroxy ketone and a tertiary alpha-hydroxy ketone. It has a role as an Escherichia coli metabolite. It is a conjugate base of a doxorubicin(1+). It derives from a hydride of a tetracene.
Structures of L-daunosamine 1, L-3-epi-daunosamine 2, L-ristosamine 3, L-acosamine 4, and the anthracycline antibiotics daunorubicin 5, doxorubicin 6, carubicin 7, idarubicin 8, and epirubicin 9.
Thymectacin, a phosphoramidate derivative of (E)-5-(2-bromovinyl)-2'-deoxyuridine, is a novel small molecule anticancer agent. Thymectacin is selectively active against tumor cells expressing high levels of thymidylate synthase (TS), a critical enzyme in DNA biosynthesis. Thymectacin was as efficacious as irinotecan, a drug recently approved for the treatment of 5-fluorouracil-resistant colon cancer.
Known ProTides: SOFOSBUVIR, GS-9131, GS-7340, Thymectacin, NUC-1031.
K-11777 is a cysteine protease inhibitor that acts as a broad-spectrum antiviral, by targeting cathepsin-mediated cell entry.
Michael acceptor inhibitors.
a) Docking pose of inhibitor 6 (magenta) superimposed with K11777 (orange) in complex with rhodesain (PDB ID: 2P7U). b) Proposed docking pose of inhibitor 6 (magenta) in complex with rhodesain.
2-Methylthiazolidine is a member of thiazolidines.
Isomeric and conformational equilibrium for 2-methylthiazolidines 8a and 8b, with selected H and [13C] NMR data; analogous oxazolidine 183a–c is shown for comparison.
Febrifugine, a quinazolinone alkaloid that inhibits P. falciparum and has antimalarial activity, is an excellent compound that can be used to block the proliferation of malarial parasites.
Cyclopropyl radical is a highly reactive organic intermediate characterized by a three-membered cyclopropane ring bearing an unpaired electron on one of the carbon atoms.
LED-mediated cyclopropane synthesis. [a] Using trans-b-methylstyrene. [b] Using cis-b-methylstyrene. [c] 20 equiv of styrene. [d] Violet LED used. Also 27% of malonate dimer by H NMR. 1[e] Using soluble ylide 1o.