Target type: biologicalprocess
Any process that activates or increases the frequency, rate or extent of transcription mediated by RNA polymerase III. [GOC:go_curators, GOC:txnOH]
Positive regulation of transcription by RNA polymerase III is a complex and essential process that controls the synthesis of a wide variety of small, non-coding RNAs. These RNAs play crucial roles in a multitude of cellular functions, including translation, ribosome biogenesis, and RNA processing. The process involves the coordinated action of numerous factors, including transcription factors, coactivators, and chromatin modifiers.
Transcription initiation by RNA polymerase III is distinct from that of RNA polymerase II, which transcribes protein-coding genes. RNA polymerase III promoters are typically located within the transcribed region of the gene, rather than upstream of it. They often contain internal control regions (ICRs), which are short sequence elements that bind specific transcription factors.
The process can be broadly divided into the following steps:
1. **Transcription Factor Binding**: Specific transcription factors, such as TFIIIA, TFIIIB, and TFIIIC, recognize and bind to the ICRs within the gene. TFIIIA binds to the 5S rRNA gene, while TFIIIB and TFIIIC bind to the tRNA gene.
2. **Assembly of the Transcription Pre-initiation Complex (PIC)**: The transcription factors bind to the DNA, forming a stable complex that recruits RNA polymerase III. This complex is referred to as the PIC.
3. **Recruitment of RNA Polymerase III**: Once the PIC is formed, RNA polymerase III is recruited to the promoter, facilitated by the interactions between TFIIIB and the polymerase.
4. **Initiation of Transcription**: RNA polymerase III initiates transcription at the start site within the promoter, producing a primary transcript.
5. **Elongation and Termination**: RNA polymerase III then transcribes the gene, elongating the RNA molecule. The process is terminated at specific termination signals, releasing the newly synthesized RNA transcript.
6. **Post-Transcriptional Modifications**: The newly transcribed RNA may undergo further processing, including capping, splicing, and polyadenylation, depending on the specific type of RNA.
The positive regulation of transcription by RNA polymerase III is tightly controlled by a variety of mechanisms, including:
* **Signal-dependent activation**: In response to various cellular signals, specific transcription factors are activated, promoting the assembly of the PIC and subsequent transcription.
* **Chromatin Remodeling**: Chromatin modifications, such as histone acetylation and methylation, can influence the accessibility of the DNA to transcription factors and RNA polymerase III.
* **Post-translational modifications of transcription factors**: Modifications of transcription factors, such as phosphorylation and acetylation, can alter their activity and influence the transcription process.
* **Interaction with other cellular factors**: Transcription factors and RNA polymerase III can interact with other cellular proteins and complexes, further regulating their activity and influencing transcription.
The positive regulation of transcription by RNA polymerase III is a complex and dynamic process that is crucial for maintaining cellular homeostasis and proper gene expression. It involves a precise interplay of various factors and regulatory mechanisms, ensuring the accurate production of essential non-coding RNAs that support diverse cellular functions.
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Protein | Definition | Taxonomy |
---|---|---|
Regulatory-associated protein of mTOR | A regulatory-associated protein of mTOR that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8N122] | Homo sapiens (human) |
Serine/threonine-protein kinase mTOR | A serine/threonine-protein kinase mTOR that is encoded in the genome of human. [PRO:CL, UniProtKB:P42345] | Homo sapiens (human) |
Androgen receptor | An androgen receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P10275] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
bicalutamide | bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism. bicalutamide: approved for treatment of advanced prostate cancer N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group. | (trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol | |
caffeine | purine alkaloid; trimethylxanthine | adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic | |
chloroquine | chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis. Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses. | aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug |
flufenamic acid | flufenamic acid : An aromatic amino acid consisting of anthranilic acid carrying an N-(trifluoromethyl)phenyl substituent. An analgesic and anti-inflammatory, it is used in rheumatic disorders. Flufenamic Acid: An anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically. (From Martindale, The Extra Pharmacopoeia, 30th ed, p16) | aromatic amino acid; organofluorine compound | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
flutamide | Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species. | (trifluoromethyl)benzenes; monocarboxylic acid amide | androgen antagonist; antineoplastic agent |
indomethacin | indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. | aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole | analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic; xenobiotic metabolite |
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source | chromones; morpholines; organochlorine compound | autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector |
entinostat | benzamides; carbamate ester; primary amino compound; pyridines; substituted aniline | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor | |
nilutamide | (trifluoromethyl)benzenes; C-nitro compound; imidazolidinone | androgen antagonist; antineoplastic agent | |
masoprocol | nordihydroguaretic acid: antioxidant compound found in the creosote bush (Larrea tridentata) | catechols; lignan; tetrol | antioxidant; ferroptosis inhibitor; geroprotector; plant metabolite |
salicylamide | salamide: a major impurity of hydrochlorothiazide; structure in first source | phenols; salicylamides | antirheumatic drug; non-narcotic analgesic |
imatinib | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor | |
prednisolone | prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states. | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic |
3,3',5-triiodothyroacetic acid | tiratricol : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)acetic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxy-3-iodophenoxy group. It is a thyroid hormone analogue that has been used in the treatment of thyroid hormone resistance syndrome. | ||
spironolactone | spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7. Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827) | 3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester | aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
oxandrolone | Oxandrolone: A synthetic hormone with anabolic and androgenic properties. | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid | anabolic agent; androgen |
triiodothyronine | 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism. Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3. | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
testosterone propionate | androgen : A sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors. Testosterone Propionate: An ester of TESTOSTERONE with a propionate substitution at the 17-beta position. | steroid ester | |
medroxyprogesterone acetate | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; corticosteroid; steroid ester | adjuvant; androgen; antineoplastic agent; antioxidant; female contraceptive drug; inhibitor; progestin; synthetic oral contraceptive | |
fluoxymesterone | Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women. | 11beta-hydroxy steroid; 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid; fluorinated steroid | anabolic agent; antineoplastic agent |
bisphenol a | 4,4'-isopropylidene diphenol: stimulates proliferative responses and cytokine productions of murine spleen cells and thymus cells in vitro bisphenol : By usage, the methylenediphenols, HOC6H4CH2C6H4OH, commonly p,p-methylenediphenol, and their substitution products (generally derived from condensation of two equivalent amounts of a phenol with an aldehyde or ketone). The term also includes analogues in the the methylene (or substituted methylene) group has been replaced by a heteroatom. bisphenol A : A bisphenol that is 4,4'-methanediyldiphenol in which the methylene hydrogens are replaced by two methyl groups. | bisphenol | endocrine disruptor; environmental contaminant; xenobiotic; xenoestrogen |
uvitex swn | Uvitex SWN: optical brightner from Ciba; structure | 7-aminocoumarins | fluorochrome |
cyproterone acetate | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; chlorinated steroid; steroid ester | androgen antagonist; geroprotector; progestin | |
flavanone | flavanone : The simplest member of the class of flavanones that consists of flavan bearing an oxo substituent at position 4. flavanone: RN given refers to cpd with unspecified isomeric designation; structure in first source | flavanones | |
androstenediol | androst-5-ene-3beta,17beta-diol : A 3beta-hydroxy-Delta(5)-steroid that is 3beta-hydroxyandrost-5-ene carrying an additional hydroxy group at position 17beta. Androstenediol: An intermediate in TESTOSTERONE biosynthesis, found in the TESTIS or the ADRENAL GLANDS. Androstenediol, derived from DEHYDROEPIANDROSTERONE by the reduction of the 17-keto group (17-HYDROXYSTEROID DEHYDROGENASES), is converted to TESTOSTERONE by the oxidation of the 3-beta hydroxyl group to a 3-keto group (3-HYDROXYSTEROID DEHYDROGENASES). | 17beta-hydroxy steroid; 3beta-hydroxy-Delta(5)-steroid | androgen; human metabolite; mouse metabolite; radiation protective agent |
dihydrotestosterone | 17beta-hydroxy-5alpha-androstan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4,5 double bond has been reduced to a single bond with alpha-configuration at position 5. 17beta-hydroxyandrostan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4-5 double bond has been reduced to a single bond with unspecified configuration at position 5. Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE. | 17beta-hydroxy steroid; 17beta-hydroxyandrostan-3-one; 3-oxo-5alpha-steroid | androgen; Daphnia magna metabolite; human metabolite; mouse metabolite |
flavone | flavone : The simplest member of the class of flavones that consists of 4H-chromen-4-one bearing a phenyl substituent at position 2. flavone: RN given refers to unlabeled cpd; structure given in first source | flavones | metabolite; nematicide |
3-hydroxyflavone | 3-hydroxyflavone: structure given in first source flavonol : A monohydroxyflavone that is the 3-hydroxy derivative of flavone. | flavonols; monohydroxyflavone | |
n-phenylpyrrole | N-phenylpyrrole: structure in first source | ||
1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane | 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane: a flame retardant and androgen receptor agonist; structure in first source | ||
raspberry ketone | raspberry ketone : A ketone that is 4-phenylbutan-2-one in which the phenyl ring is substituted at position 4 by a hydroxy group. It is found in a variety of fruits including raspberries, blackberries and cranberries, and is used in perfumery and cosmetics. rheosmin: an NSAID that blocks NF-kappaB activation; isolated from Pinus densiflora; structure in first source | methyl ketone; phenols | androgen antagonist; cosmetic; flavouring agent; fragrance; hepatoprotective agent; metabolite |
zingerone | zingerone : A methyl ketone that is 4-phenylbutan-2-one in which the phenyl ring is substituted at positions 3 and 4 by methoxy and hydroxy groups respectively. The major pungent component in ginger. zingerone: pungent principle of ginger; structure | methyl ketone; monomethoxybenzene; phenols | anti-inflammatory agent; antiemetic; antioxidant; flavouring agent; fragrance; plant metabolite; radiation protective agent |
staurosporine | indolocarbazole alkaloid; organic heterooctacyclic compound | apoptosis inducer; bacterial metabolite; EC 2.7.11.13 (protein kinase C) inhibitor; geroprotector | |
mifepristone | Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
nitrogenase stabilizing-protective protein, bacteria | N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide | androgen antagonist; antineoplastic agent | |
5-hydroxyflavone | flavones | ||
4(5)-phenylimidazole | 4(5)-phenylimidazole: tautomeric cpd; cytochrome P450 14alpha-sterol demethylase, CYP51 antagonist | ||
2-phenylimidazole | |||
2-(2'-pyridyl)benzimidazole | 2-(2'-pyridyl)benzimidazole: structure in first source | ||
6-hydroxyflavone | 6-hydroxyflavone: antioxidant; structure in first source | hydroxyflavonoid | |
1-phenylimidazole | 1-phenylimidazole: ligand for cytochrome P-450 & inhibitor of microsomal oxidation | ||
hydroxyflutamide | |||
5-Methoxyflavone | 5-methoxyflavone: DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity; structure in first source | ether; flavonoids | |
6-methoxyflavanone | 6-methoxyflavanone: structure in first source | ||
gefitinib | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist | |
lestaurtinib | indolocarbazole | ||
5,5-dimethyl-3-(alpha,alpha,alpha,4-tetrafluoro-3-tolyl)hydantoin | 5,5-dimethyl-3-(alpha,alpha,alpha,4-tetrafluoro-3-tolyl)hydantoin: structure given in first source | ||
4-(3,4,4-trimethyl-5-oxo-2-thioxo-1-imidazolidinyl)-2-(trifluoromethyl)benzonitrile | 4-(3,4,4-trimethyl-5-oxo-2-thioxo-1-imidazolidinyl)-2-(trifluoromethyl)benzonitrile: a non-steroidal antiandrogen; structure given in first source | ||
ru 58841 | |||
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(+-)-isomer | |||
6-methoxyflavone | 6-methoxyflavone: suppresses NFAT-mediated T cell activation; structure in first source | ether; flavonoids | |
vatalanib | monochlorobenzenes; phthalazines; pyridines; secondary amino compound | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; vascular endothelial growth factor receptor antagonist | |
ruboxistaurin | ruboxistaurin: inhibits protein kinase C beta; structure in first source | ||
canertinib | monochlorobenzenes; morpholines; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor | |
birb 796 | aromatic ether; morpholines; naphthalenes; pyrazoles; ureas | EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; immunomodulator | |
2'-hydroxyflavone | 2'-hydroxyflavone: isolated from Daphnopsis sellowiana; structure given in first source | flavones | |
triptophenolide | triptophenolide: structure given in first source | oxo steroid | |
sb 203580 | imidazoles; monofluorobenzenes; pyridines; sulfoxide | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent | |
enzastaurin | indoles; maleimides | ||
erlotinib | aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound | antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor | |
2'-hydroxyflavanone | |||
lapatinib | furans; organochlorine compound; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor | |
sorafenib | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide | angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor | |
6-chloroflavone | 6-chloroflavone: structure in first source | ||
metribolone | 17beta-hydroxy-17-methylestra-4,9,11-trien-3-one : A synthetic non-aromatisable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors. Metribolone: A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors. | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid | androgen |
wortmannin | acetate ester; cyclic ketone; delta-lactone; organic heteropentacyclic compound | anticoronaviral agent; antineoplastic agent; autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector; Penicillium metabolite; radiosensitizing agent | |
(S)-bicalutamide | (S)-bicalutamide : A N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide that is the (S)-enantiomer of bicalutamide. | N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide | |
eplerenone | Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION. | 3-oxo-Delta(4) steroid; epoxy steroid; gamma-lactone; methyl ester; organic heteropentacyclic compound; oxaspiro compound; steroid acid ester | aldosterone antagonist; antihypertensive agent |
3-(3-pyridyl)-1-propyl-(2s)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate | |||
tacrolimus | tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro. | macrolide lactam | bacterial metabolite; immunosuppressive agent |
pd 173955 | PD 173955: inhibits src family-selective tyrosine kinase; structure in first source | aryl sulfide; dichlorobenzene; methyl sulfide; pyridopyrimidine | tyrosine kinase inhibitor |
7-methoxyflavone | 7-methoxyflavone: an aromatase inhibitor | ether; flavonoids | |
2-(2-phenoxyethylsulfonyl)-1H-benzimidazole | benzimidazoles; sulfoxide | ||
tolfenamic acid | tolfenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 3-chloro-2-methylphenyl group. Tolfenamic acid is used specifically for relieving the pain of migraine. It also shows anticancer activity. tolfenamic acid: structure | aminobenzoic acid; organochlorine compound; secondary amino compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; EC 2.7.1.33 (pantothenate kinase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
cgp 60474 | substituted aniline | ||
s 1033 | (trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor | |
N-(4-phenylmethoxyphenyl)methanesulfonamide | sulfonamide | ||
3,6-dihydroxyflavone | 3,6-dihydroxyflavone: induces apoptosis in leukemia HL-60 cells; structure in first source | ||
6-methylflavone | 6-methylflavone: structure in first source | ||
7-benzyloxy-4-trifluoromethylcoumarin | 7-benzyloxy-4-trifluoromethylcoumarin: a substrate for CYP3A4 | ||
6-hydroxyflavanone | 6-hydroxyflavanone : A monohydroxyflavanone that is flavanone substituted by a hydroxy group at position 6. | monohydroxyflavanone | fungal xenobiotic metabolite |
bms 387032 | N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide: a CDK2 inhibitor with antineoplastic activity; structure in first source N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of piperidine-4-carboxylic acid with the amino group of 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-amine. It is an ATP-competitive inhibitor of CDK2, CDK7 and CDK9 kinases and exhibits anti-cancer properties. | 1,3-oxazoles; 1,3-thiazoles; organic sulfide; piperidinecarboxamide; secondary carboxamide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
tandutinib | aromatic ether; N-arylpiperazine; N-carbamoylpiperazine; phenylureas; piperidines; quinazolines; tertiary amino compound | antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | |
vx-745 | aryl sulfide; dichlorobenzene; difluorobenzene; pyrimidopyridazine | anti-inflammatory drug; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | |
dasatinib | dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source | 1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
zd 6474 | CH 331: structure in first source | aromatic ether; organobromine compound; organofluorine compound; piperidines; quinazolines; secondary amine | antineoplastic agent; tyrosine kinase inhibitor |
epi 001 | bisphenol A (3-chloro-2-hydroxypropyl) (2,3-dihydroxypropyl) ether : The (3-chloro-2-hydroxypropyl) (2,3-dihydroxypropyl) diether of bisphenol A; a small molecule that inhibits transactivation of the AR amino-terminal domain (NTD). EPI 001: an antineoplastic agent and androgen receptor antagonist; structure in first source | diether; organochlorine compound | androgen antagonist |
ku 55933 | 2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one: specific inhibitor of the ataxia-telangiectasia mutated kinase ATM; structure in first source | ||
biochanin a | 4'-methoxyisoflavones; 7-hydroxyisoflavones | antineoplastic agent; EC 3.5.1.99 (fatty acid amide hydrolase) inhibitor; phytoestrogen; plant metabolite; tyrosine kinase inhibitor | |
acacetin | 5,7-dihydroxy-4'-methoxyflavone : A monomethoxyflavone that is the 4'-methyl ether derivative of apigenin. | dihydroxyflavone; monomethoxyflavone | anticonvulsant; plant metabolite |
apigenin | Chamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia. | trihydroxyflavone | antineoplastic agent; metabolite |
luteolin | 3'-hydroxyflavonoid; tetrahydroxyflavone | angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; c-Jun N-terminal kinase inhibitor; EC 2.3.1.85 (fatty acid synthase) inhibitor; immunomodulator; nephroprotective agent; plant metabolite; radical scavenger; vascular endothelial growth factor receptor antagonist | |
calcitriol | dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | D3 vitamins; hydroxycalciol; triol | antineoplastic agent; antipsoriatic; bone density conservation agent; calcium channel agonist; calcium channel modulator; hormone; human metabolite; immunomodulator; metabolite; mouse metabolite; nutraceutical |
kaempferol | 7-hydroxyflavonol; flavonols; tetrahydroxyflavone | antibacterial agent; geroprotector; human blood serum metabolite; human urinary metabolite; human xenobiotic metabolite; plant metabolite | |
genistein | 7-hydroxyisoflavones | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; geroprotector; human urinary metabolite; phytoestrogen; plant metabolite; tyrosine kinase inhibitor | |
pyrvinium | pyrvinium : A quinolinium ion that is 1-methylquinolinium substituted by dimethylamino group at position 6 and a (E)-2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl at position 2. It is a anthelminthic drug active against pinworms. The salts of pyrvinium can also be used as anticancer agents. pyrvinium: RN given refers to parent cpd; synonyms vanquin & vankin refer to pamoate[2:1]; structure in Merck Index, 9th ed, #7810 | quinolinium ion | anthelminthic drug; antineoplastic agent |
baicalein | trihydroxyflavone | angiogenesis inhibitor; anti-inflammatory agent; antibacterial agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antioxidant; apoptosis inducer; EC 1.13.11.31 (arachidonate 12-lipoxygenase) inhibitor; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; EC 4.1.1.17 (ornithine decarboxylase) inhibitor; ferroptosis inhibitor; geroprotector; hormone antagonist; plant metabolite; prostaglandin antagonist; radical scavenger | |
chrysin | chrysin : A dihydroxyflavone in which the two hydroxy groups are located at positions 5 and 7. | 7-hydroxyflavonol; dihydroxyflavone | anti-inflammatory agent; antineoplastic agent; antioxidant; EC 2.7.11.18 (myosin-light-chain kinase) inhibitor; hepatoprotective agent; plant metabolite |
galangin | 5,7-dihydroxyflavonol: antimicrobial from the twigs of Populus nigra x Populus deltoides; structure in first source galangin : A 7-hydroxyflavonol with additional hydroxy groups at positions 3 and 5 respectively; a growth inhibitor of breast tumor cells. | 7-hydroxyflavonol; trihydroxyflavone | antimicrobial agent; EC 3.1.1.3 (triacylglycerol lipase) inhibitor; plant metabolite |
daidzein | 7-hydroxyisoflavones | antineoplastic agent; EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; phytoestrogen; plant metabolite | |
prunetin | prunetin : A hydroxyisoflavone that is genistein in which the hydroxy group at position 7 is replaced by a methoxy group. prunetin: reduces herpes virus-1 plaque formation | 7-methoxyisoflavones; hydroxyisoflavone | anti-inflammatory agent; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor; metabolite |
7-hydroxyflavone | 7-hydroxyflavone : A hydroxyflavonoid in which the flavone nucleus is substituted at position 7 by a hydroxy group. | hydroxyflavonoid | |
dorzolamide | dorzolamide : 5,6-Dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide in which hydrogens at the 4 and 6 positions are substituted by ethylamino and methyl groups, respectively (4S, trans-configuration). A carbonic anhydrase inhibitor, it is used as the hydrochloride in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension. dorzolamide: topically effective ocular hypotensive carbonic anhydrase inhibitor; RN refers to mono-HCl (4S-trans)-isomer | sulfonamide; thiophenes | antiglaucoma drug; antihypertensive agent; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
sirolimus | sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent. Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties. | antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol | antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor |
alvocidib | alvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation. alvocidib: structure given in first source | dihydroxyflavone; hydroxypiperidine; monochlorobenzenes; tertiary amino compound | antineoplastic agent; antirheumatic drug; apoptosis inducer; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
onapristone | onapristone: induces vaginal bleeding and luteal regression in monkeys; structure given in first source; progesterone antagonist | ||
4-methylesculetin | 4-methylesculetin: has antiinflammatory activity 6,7-dihydroxy-4-methylcoumarin : A hydroxycoumarin that is 4-methylcuomarin which is substituted by hydroxy groups at positions 3 and 4. A hyaluronan synthesis inhibitor. It has also been used as a fluorescent sensor to monitor the consumption of a boronic acid in Suzuki coupling reactions; fluorescence is readily detectable by the naked eye using a standard 365 nm UV lamp. | hydroxycoumarin | anti-inflammatory agent; antioxidant; hyaluronan synthesis inhibitor |
bosutinib | 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source | aminoquinoline; aromatic ether; dichlorobenzene; N-methylpiperazine; nitrile; tertiary amino compound | antineoplastic agent; tyrosine kinase inhibitor |
su 11248 | monocarboxylic acid amide; pyrroles | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist | |
norbinaltorphimine | norbinaltorphimine: kappa opiate receptor antagonist; structure given in first source | isoquinolines | |
vx680 | N-arylpiperazine | ||
pregna-4,17-diene-3,16-dione | pregna-4,17-diene-3,16-dione: steroid from guggulu extract; RN & N1 from C1 Form index; RN given refers to cpd without isomeric designation; structure in first source; antagonist of farnesoid X receptor | 3-hydroxy steroid | androgen |
everolimus | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor | |
pregna-4,17-diene-3,16-dione, (17z)-isomer | |||
axitinib | aryl sulfide; benzamides; indazoles; pyridines | antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist | |
tetrahydrogestrinone | 3-hydroxy steroid | ||
temsirolimus | macrolide lactam | ||
pd 184352 | 2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide: inhibits MAP kinase kinase; structure in first source | aminobenzoic acid | |
lonaprisan | lonaprisan: structure in first source | ||
asoprisnil | asoprisnil: structure in first source | ||
zk 216348 | ZK 216348: ZK-209614 is the racemic mixture, ZK-216348 is the (+)-isomer, and ZK-216347 is the (-)-isomer; a selective glucocorticoid receptor agonist; structure in first source | ||
bms345541 | 4(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline: structure in first source | quinoxaline derivative | |
abiraterone acetate | abiraterone acetate : A sterol ester obtained by formal condensation of the 3-hydroxy group of abiraterone with the carboxy group of acetic acid. A prodrug that is converted in vivo into abiraterone. Used for treatment of metastatic castrate-resistant prostate cancer. Abiraterone Acetate: An androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER. | pyridines; sterol ester | antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor; prodrug |
andarine | acetamides; anilide | ||
17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | |||
midostaurin | midostaurin : An organic heterooctacyclic compound that is the N-benzoyl derivative of staurosporine. | benzamides; gamma-lactam; indolocarbazole; organic heterooctacyclic compound | antineoplastic agent; EC 2.7.11.13 (protein kinase C) inhibitor |
trestolone | trestolone: structure given in first source; RN given refers to (7alpha,17beta)-isomer | ||
lg 121071 | |||
px-866 | PX-866 : An organic heterotetracyclic compound that is obtained from wortmanin via aminolysis of its furan ring by diallyl amine. PX-866: inhibitor of phosphoinositide-3-kinase signaling with antitumor activity; structure in first source | acetate ester; delta-lactone; organic heterotetracyclic compound; tertiary amino compound | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
nu 7026 | 2-(morpholin-4-yl)benzo(h)chromen-4-one: a radiosensitizing agent that inhibits DNA-dependent protein kinase; structure in first source | organic heterotricyclic compound; organooxygen compound | |
17-hydroxywortmannin | 17-hydroxywortmannin: inhibits secretion of human neutrophils | ||
ki 20227 | |||
zotarolimus | zotarolimus: synthetic analog of rapamycin; structure in first source | lactam; macrolide | |
bms-564929 | |||
pi103 | PI103: pyridofuropyrimidine antineoplastic; a potent inhibitor of class I phosphatidylinositide 3-kinases (PI3K); structure in first soruce | aromatic amine; morpholines; organic heterotricyclic compound; phenols; tertiary amino compound | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor |
PI3-Kinase alpha Inhibitor 2 | organic heterobicyclic compound; organonitrogen heterocyclic compound; organosulfur heterocyclic compound | ||
hki 272 | nitrile; quinolines | antineoplastic agent; tyrosine kinase inhibitor | |
tofacitinib | tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis. | N-acylpiperidine; nitrile; pyrrolopyrimidine; tertiary amino compound | antirheumatic drug; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor |
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | |||
cediranib | aromatic ether | ||
way-362450 | indoles | ||
masitinib | 1,3-thiazoles; benzamides; N-alkylpiperazine; pyridines | antineoplastic agent; antirheumatic drug; tyrosine kinase inhibitor | |
pazopanib | pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer. pazopanib: a protein kinase inhibitor | aminopyrimidine; indazoles; sulfonamide | angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist |
azd 6244 | AZD 6244: a MEK inhibitor | benzimidazoles; bromobenzenes; hydroxamic acid ester; monochlorobenzenes; organofluorine compound; secondary amino compound | anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor |
su 14813 | 5-((5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl)-N-(2-hydroxy-3-morpholin-4-ylpropyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide: has both antineoplastic and antiangiogenic activities; structure in first source | ||
bibw 2992 | aromatic ether; enamide; furans; monochlorobenzenes; organofluorine compound; quinazolines; secondary carboxamide; tertiary amino compound | antineoplastic agent; tyrosine kinase inhibitor | |
tg100-115 | 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol: for treatment of ischemia reperfusion injury; structure in first source | pteridines | |
pha 665752 | dichlorobenzene; enamide; indolones; N-acylpyrrolidine; pyrrolecarboxamide; secondary carboxamide; sulfone; tertiary carboxamide | antineoplastic agent; c-Met tyrosine kinase inhibitor | |
3beta-hydroxy-17-(1h-benzimidazole-1-yl)androsta-5,16-diene | 3-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene: has antineoplastic activity; structure in first source | 3-hydroxy steroid | androgen |
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | methoxybenzenes; substituted aniline | ||
brivanib | aromatic ether; diether; fluoroindole; pyrrolotriazine; secondary alcohol | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; drug metabolite; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; fibroblast growth factor receptor antagonist | |
mk 2866 | |||
nu 7441 | 8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one: structure in first source | dibenzothiophenes | |
at 7519 | 4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-pyrazole-3-carboxamide : A member of the class of pryrazoles that is 4-amino-1H-pyrazole-3-carboxylic acid in which the primary amino group has been acylated by a 2,6-dichlorobenzoyl group and in which the carboxylic acid has been converted into a carboxamide by formal condensation with the primary amino group of 4-aminopiperidine. | dichlorobenzene; piperidines; pyrazoles; secondary carboxamide | antineoplastic agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
bi 2536 | |||
nvp-ast487 | NVP-AST487: antineoplastic; a RET kinase inhibitor that blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells | ||
kw 2449 | KW 2449: has both multikinase inhibitory activity and antineoplastic activity; structure in first source | ||
abt 869 | aromatic amine; indazoles; phenylureas | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | |
lgd 2226 | |||
gw 2580 | 5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine: a cFMS kinase inhibitor; structure in first source | ||
idelalisib | idelalisib : A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia. idelalisib: an antineoplastic agent and p110delta inhibitor; structure in first source | aromatic amine; organofluorine compound; purines; quinazolines; secondary amino compound | antineoplastic agent; apoptosis inducer; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
crizotinib | crizotinib : A 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine that has R configuration at the chiral centre. The active enantiomer, it acts as a kinase inhibitor and is used for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) Crizotinib: A piperidine and aminopyridine derivative that acts as an inhibitor of RECEPTOR PROTEIN-TYROSINE KINASES, including ANAPLASTIC LYMPHOMA KINASE (ALK) and HEPATOCYTE GROWTH FACTOR RECEPTOR (HGFR; c-Met). It is used in the treatment of NON-SMALL CELL LUNG CANCER. | 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | antineoplastic agent; biomarker; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor |
zstk474 | ZSTK-474 : A triamino-1,3,5-triazine that is 1,3,5-triazine in which two of the hydrogens have been replaced by morpholin-4-yl groups while the third hydrogen has been replaced by a 2-(difluoromethyl)benzimidazol-1-yl group. It is an inhibitor of phosphatidylinositol 3-kinase. | benzimidazoles; morpholines; organofluorine compound; triamino-1,3,5-triazine | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
chir-265 | aromatic ether | ||
motesanib | pyridinecarboxamide | ||
mln8054 | benzazepine | ||
GDC-0879 | indanes; ketoxime; primary alcohol; pyrazoles; pyridines | antineoplastic agent; B-Raf inhibitor | |
ku-0060648 | dibenzothiophenes | ||
dactolisib | dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment. dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR | imidazoquinoline; nitrile; quinolines; ring assembly; ureas | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor |
lg190155 | LG190155: structure in first source | ||
lg190178 | |||
mdv 3100 | (trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound | androgen antagonist; antineoplastic agent | |
gsk 461364 | GSK 461364: an antineoplastic agent that inhibits polo-like kinase 1 | (trifluoromethyl)benzenes | |
azd 1152-hqpa | AZD2811: has antineoplastic activity; structure in first source | anilide; monofluorobenzenes; primary alcohol; pyrazoles; quinazolines; secondary amino compound; secondary carboxamide; tertiary amino compound | antineoplastic agent; Aurora kinase inhibitor |
nvp-tae684 | piperidines | ||
2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | pyrazolopyridine | ||
buparlisib | NVP-BKM120: a pan class I PI3 kinase inhibitor with antineoplastic activity; structure in first source | aminopyridine; aminopyrimidine; morpholines; organofluorine compound | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
fedratinib | fedratinib: a selective small-molecule inhibitor of JAK2 | sulfonamide | |
gsk690693 | 1,2,5-oxadiazole; acetylenic compound; aromatic amine; aromatic ether; imidazopyridine; piperidines; primary amino compound; tertiary alcohol | antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | |
way 252623 | 2-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole: a partial LXR agonist | ||
ku 0063794 | Ku 0063794: an mTOR inhibitor; structure in first source | benzyl alcohols; monomethoxybenzene; morpholines; pyridopyrimidine; tertiary amino compound | antineoplastic agent; mTOR inhibitor |
gdc 0941 | pictrelisib : A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring. | indazoles; morpholines; piperazines; sulfonamide; thienopyrimidine | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
plx 4720 | PLX 4720: a B-Raf(V600E) kinase inhibitor; structure in first source | aromatic ketone; difluorobenzene; organochlorine compound; pyrrolopyridine; sulfonamide | antineoplastic agent; B-Raf inhibitor |
sgx 523 | aryl sulfide; biaryl; pyrazoles; quinolines; triazolopyridazine | c-Met tyrosine kinase inhibitor; nephrotoxic agent | |
apalutamide | |||
quizartinib | benzoimidazothiazole; isoxazoles; morpholines; phenylureas | antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; necroptosis inhibitor | |
PP121 | aromatic amine; cyclopentanes; pyrazolopyrimidine; pyrrolopyridine | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; tyrosine kinase inhibitor | |
pf-04691502 | |||
pf 998425 | |||
incb-018424 | nitrile; pyrazoles; pyrrolopyrimidine | antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | |
gsk 2126458 | omipalisib : A member of the class of quinolines that is quinoline which is substituted by pyridazin-4-yl and 5-[(2,4-difluorobenzene-1-sulfonyl)amino]-6-methoxypyridin-3-yl groups at positions 4 and 6, respectively. It is a highly potent inhibitor of PI3K and mTOR developed by GlaxoSmithKline and was previously in human phase 1 clinical trials for the treatment of idiopathic pulmonary fibrosis and solid tumors. omipalisib: inhibitor of mTOR protein | aromatic ether; difluorobenzene; pyridazines; pyridines; quinolines; sulfonamide | anticoronaviral agent; antineoplastic agent; autophagy inducer; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor; radiosensitizing agent |
gsk 1838705a | organonitrogen compound; organooxygen compound | ||
lgd 3303 | 9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo(3,2-f)quinolin-7(6H)-one: an androgen receptor modulator; structure in first source | ||
gne 477 | GNE 477: inhibits phosphatidylinositol 3-kinase and mTOR; structure in first source | ||
gdc 0980 | |||
wye 125132 | WYE 125132: an antineoplastic agent that inhibits mTORC1 and mTORC2 | ureas | |
azd2014 | vistusertib: potent and selective dual mTORC1 and mTORC2 inhibitor; structure in first source | ||
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | (5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol: a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity; structure in first source | benzyl alcohols; morpholines; pyridopyrimidine; tertiary amino compound | antineoplastic agent; apoptosis inducer; mTOR inhibitor |
gsk 1363089 | GSK 1363089: a multikinase inhibitor that acts on Met, RON, Axl, and VEGFR; structure in first source | aromatic ether | |
pki 402 | PKI 402: also inhibits mammalian target of rapamycin; structure in first source | ||
4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester | WYE-354: an mTOR inhibitor; structure in first source | carbamate ester | |
nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source | ||
pki 587 | gedatolisib: inhibits both phosphatidylinositol 3-kinase and mTOR; structure in first source | ||
cp 466722 | quinazolines | ||
CAY10626 | ureas | ||
5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | sapanisertib: an mTOR inhibitor | benzoxazole | |
(3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)-4-pyrimidinyl]-3-methylmorpholine | indoles | ||
pf-03882845 | |||
azd3514 | AZD3514: in Phase I clinical trial in patients with castrate-resistant prostate cancer (2/2013); structure in first source | ||
etp-46321 | ETP-46321: inhibits PI3K alpha and PI3K delta; structure in first source | ||
ch 5132799 | CH 5132799: structure in first source | ||
torin 1 | torin 1 : A member of the class of pyridoquinolines that is 9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2-one bearing an additional 4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl substituent at position 1. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. | N-acylpiperazine; N-arylpiperazine; organofluorine compound; pyridoquinoline; quinolines | antineoplastic agent; mTOR inhibitor |
gdc-0032 | |||
pf-4989216 | PF-4989216: inhibits phosphatidylinositol 3-kinase; structure in first source | ||
torin 2 | torin 2 : A member of the class of pyridoquinolines that is benzo[h][1,6]naphthyridin-2-one carrying additional 3-(trifluoromethyl)phenyl and 6-aminopyridin-3-yl substituents at positions 1 and 9 respectively. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. | aminopyridine; organofluorine compound; primary amino compound; pyridoquinoline | antineoplastic agent; mTOR inhibitor |
cudc-907 | |||
sar245408 | |||
byl719 | proline derivative | ||
amg 511 | AMG 511: structure in first source | ||
cc214-2 | CC214-2: an mTOR kinase inhibitor; structure in first source | ||
cc-223 | |||
cc-115 | 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino(2,3-b)pyrazin-2(1H)-one: an mTOR kinase inhibitor; structure in first source | ||
bay 94-8862 | finerenone: a potent, selective, and orally available nonsteroidal mineralocorticoid receptor antagonist; structure in first source | ||
gne-317 | GNE-317: an mTOR inhibitor also; structure in first source | ||
etp-46464 | ETP-46464: inhibits ATM and Rad3-related kinase; structure in first source | ||
sar405 | SAR405: a Vps34 inhibitor with antineoplastic activity; structure in first source | ||
azd9496 | AZD9496: an estrogen receptor antagonist; structure in first source | ||
chir 258 | |||
nintedanib | nintedanib : A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer. | ||
bay 80-6946 | copanlisib : An imidazoquinazoline that is 2,3-dihydroimidazo[1,2-c]quinazoline substituted by (2-aminopyrimidine-5-carbonyl)amino, methoxy, and 3-(morpholin-4-yl)propoxy groups at positions 5, 7 and 8, respectively. It is a intravenous pan-class I PI3K inhibitor used for the treatment of relapsed follicular lymphoma in patients who have received at least 2 prior systemic therapies. copanlisib: an antineoplastic agent with PI3K inhibitory activity; structure in first source | ||
pp242 | torkinib : A member of the class of pyrazolopyrimidines that is 1H-pyrazolo[3,4-d]pyrimidine substituted by isopropyl, 5-hydroxyindol-2-yl and amino groups at positions 1, 3 and 4 respectively. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. | aromatic amine; biaryl; hydroxyindoles; phenols; primary amino compound; pyrazolopyrimidine | antineoplastic agent; mTOR inhibitor |