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Natural Products - NF-kB Pathway Inhibitors
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ALX-350-258 Revised 08-Apr-08
Parthenolide
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SYNONYMS (1aR-[1aR*,4E,7aS*,-10aS*,-10bR*])-2,3-6,7,7a,8,10a,10b-Octahydro-1a,5-dimethyl-8-methyleneoxireno[9,10]cyclo deca[1,2-b]furan-9(1aH)-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-258-M005   5 mg 15.00 USD Add To Cart
ALX-350-258-M025   25 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C15H20O3
MW: 248.3
CAS NUMBER: 20554-84-1
MERCK INDEX: 14: 7048
RTECS: LY4220000
SOURCE/HOST: Isolated from feverfew leaves.
PURITY: ≥99% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (100mg/ml), dichloromethane (50mg/ml) or 100% ethanol (20mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Sesquiterpene lactone. Anti-inflammatory compound. Specifically inhibits activation of NF-κB by preventing the degradation of IκBα and IκBβ. Inhibits activation of MAP kinase (MAPK/ERK) and generation of leukotriene B4 and thromboxane B2. Potent anticancer agent. Induces apoptosis in various cancer cell lines. Specifically inhibits histone deacetylase 1 (HDAC1) without affecting other class I/II HDACs. Inhibits tubulin carboxypeptidase (TCP) activity.

Product Specific Literature References
A comparison of the effects of an extract of feverfew and parthenolide, a component of feverfew, on human platelet activity in-vitro: W.A. Groenewegen & S. Heptinstall; J. Pharm. Pharmacol. 42, 553 (1990) Abstract
Feverfew extracts and parthenolide irreversibly inhibit vascular responses of the rabbit aorta: R.W. Barsby, et al.; J. Pharm. Pharmacol. 44, 737 (1992) Abstract
Inhibition of 5-lipoxygenase and cyclo-oxygenase in leukocytes by feverfew. Involvement of sesquiterpene lactones and other components: H. Sumner, et al.; Biochem. Pharmacol. 43, 2313 (1992) Abstract
Inhibition of the expression of inducible cyclooxygenase and proinflammatory cytokines by sesquiterpene lactones in macrophages correlates with the inhibition of MAP kinases: D. Hwang, et al.; BBRC 226, 810 (1996) Abstract
Sesquiterpene lactones specifically inhibit activation of NF-kappa B by preventing the degradation of I kappa B-alpha and I kappa B-beta: S.P. Hehner, et al.; J. Biol. Chem. 273, 1288 (1998) Abstract
Sesquiterpene lactones inhibit inducible nitric oxide synthase gene expression in cultured rat aortic smooth muscle cells: H.R. Wong & I.Y. Menendez; BBRC 262, 375 (1999) Abstract
The antiinflammatory sesquiterpene lactone parthenolide inhibits NF- kappa B by targeting the I kappa B kinase complex: S.P. Hehner, et al.; J. Immunol. 163, 5617 (1999) Abstract
Paclitaxel sensitivity of breast cancer cells with constitutively active NF-kappaB is enhanced by IkappaBalpha super-repressor and parthenolide: N.M. Patel, et al.; Oncogene 19, 4159 (2000) Abstract
Antitumor agent parthenolide reverses resistance of breast cancer cells to tumor necrosis factor-related apoptosis-inducing ligand through sustained activation of c-Jun N-terminal kinase: H. Nakshatri, et al.; Oncogene 23, 7330 (2004) Abstract
Involvement of proapoptotic Bcl-2 family members in parthenolide-induced mitochondrial dysfunction and apoptosis: S. Zhang, et al.; Cancer Lett. 211, 175 (2004) Abstract
Parthenolide-induced apoptosis in multiple myeloma cells involves reactive oxygen species generation and cell sensitivity depends on catalase activity: W. Wang, et al.; Apoptosis 11, 2225 (2006) Abstract
Parthenolide inhibits tubulin carboxypeptidase activity: X. Fonrose, et al.; Cancer Res. 67, 3371 (2007) Abstract
Parthenolide specifically depletes histone deacetylase 1 protein and induces cell death through ataxia telangiectasia mutated: Y.N. Gopal, et al.; Chem. Biol. 14, 813 (2007) Abstract
 
 
ALX-385-034 Revised 01-Dec-08 New product
Pterostilbene
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SYNONYMS trans-3,5-Dimethoxy-4’-hydroxystilbene
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-385-034-M025   25 mg 90.00 USD Add To Cart
ALX-385-034-M100   100 mg 270.00 USD Add To Cart
ALX-385-034-M500   500 mg 750.00 USD Add To Cart
Product Specification
FORMULA: C16H16O3
MW: 256.3
CAS NUMBER: 537-42-8
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to light brown powder.
SOLUBILITY: Soluble in DMSO (20mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and oxygen.
HAZARD: IRRITANT.
IDENTITY: Identity determined by MS and 1H-NMR.
MELTINGPOINT: 92.7-94.6°C

Product Description
Cell permeable natural methoxylated analog of resveratrol (Prod. No. ALX-270-125). Antioxidant, antiproliferative, anti-inflammatory, anti-hyperglycemic and anti-diabetic agent. Induces apoptosis. Inhibits activator protein 1 (AP-1) and NF-κB activation. Moderately inhibits COX-1 and COX-2 (IC50=19.8μM and 83.9μM).
Product Specific Literature References
Antihyperglycemic activity of phenolics from Pterocarpus marsupium: M Manickam, et al.; J. Nat. Prod. 60, 609 (1997) Abstract
Cancer chemopreventive and antioxidant activities of pterostilbene, a naturally occurring analogue of resveratrol: A.M. Rimando, et al.; J. Agric. Food Chem. 50, 3453 (2002) Abstract
Synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents: M. Roberti, et al.; J. Med. Chem. 46, 3546 (2003) Abstract
Antioxidant activity of hydroxystilbene derivatives in homogeneous solution: R. Amorati, et al.; J. Org. Chem. 69, 7101 (2004) Abstract
Association between pterostilbene and quercetin inhibits metastatic activity of B16 melanoma: P. Ferrer, et al.; Neoplasia 7, 37 (2005) Abstract; Full Text
Pterostilbene, a new agonist for the peroxisome proliferator-activated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters: A.M. Rimando, et al.; J. Agric. Food Chem. 53, 3403 (2005) Abstract
Selective COX-2 inhibition by a Pterocarpus marsupium extract characterized by pterostilbene, and its activity in healthy human volunteers: S. Hougee, et al.; Planta Med. 71, 387 (2005) Abstract
Effect of pterostilbene on hepatic key enzymes of glucose metabolism in streptozotocin- and nicotinamide-induced diabetic rats: L. Pari & M.A. Satheesh; Life Sci. 79, 641 (2006) Abstract
Effect of natural analogues of trans-resveratrol on cytochromes P4501A2 and 2E1 catalytic activities: R. Mikstacka, et al.; Xenobiotica 36, 269 (2006) Abstract
The antioxidant role of pterostilbene in streptozotocin-nicotinamide-induced type 2 diabetes mellitus in Wistar rats: M. Amarnath Satheesh & L. Pari; J. Pharm. Pharmacol. 58, 1483 (2006) Abstract
Pharmacometrics of stilbenes: seguing towards the clinic: K.A. Roupe, et al.; Curr. Clin. Pharmacol. 1, 81 (2006) Abstract
Nitric oxide mediates natural polyphenol-induced Bcl-2 down-regulation and activation of cell death in metastatic B16 melanoma: P. Ferrer, et al.; J. Biol. Chem. 282, 2880 (2007) Abstract; Full Text
Pterostilbene, an active constituent of blueberries, suppresses aberrant crypt foci formation in the azoxymethane-induced colon carcinogenesis model in rats: N. Suh, et al.; Clin. Cancer Res. 13, 350 (2007) Abstract; Full Text
Pterostilbene induces apoptosis and cell cycle arrest in human gastric carcinoma cells: M.H. Pan, et al.; J. Agric. Food Chem. 55, 7777 (2007) Abstract
Pharmacometrics of pterostilbene: preclinical pharmacokinetics and metabolism, anticancer, antiinflammatory, antioxidant and analgesic activity: C.M. Remsberg, et al.; Phytother. Res. 22, 169 (2008) Abstract
Identification of molecular pathways affected by pterostilbene, a natural dimethylether analog of resveratrol: Z. Pan, et al.; BMC Med. Genomics 1, 7 (2008) Abstract; Full Text
Pterostilbene is equally potent as resveratrol in inhibiting 12-O-tetradecanoylphorbol-13-acetate activated NFkappaB, AP-1, COX-2, and iNOS in mouse epidermis: M. Cichocki, et al.; Mol. Nutr. Food Res. 52, S62 (2008) Abstract
Pterostilbene suppressed lipopolysaccharide-induced up-expression of iNOS and COX-2 in murine macrophages: M.H. Pan, et al.; J. Agric. Food Chem. 56, 7502 (2008) Abstract
In vitro evaluation of the cytotoxic and anti-proliferative properties of resveratrol and several of its analogs: B. Billack, et al.; Cell. Mol. Biol. Lett. 13, 553 (2008) Abstract
Related Products
 
 
ALX-350-121 Revised 14-Mar-08
Rocaglamide
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SYNONYMS Rocaglamide A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - NF-kB Pathway Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-121-C100   100 µg 220.00 USD Add To Cart
Product Specification
FORMULA: C29H31NO7
MW: 505.6
CAS NUMBER: 84573-16-0
SOURCE/HOST: Isolated from Aglaia sp.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white sticky solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Immunosuppressant. Potent inhibitor of NF-κB activation in T cells, with an almost complete inhibition at 200nM. Suppresses cytokine production (IFN-γ, TNF-α, IL-2 and IL-4) and inhibits NF-AT in peripheral blood T cells at concentrations that do not impair NF-κB and AP-1 activities. In contrast to the immunosuppressant cyclosporin A (Prod. No. ALX-380-002), rocaglamide does not inhibit calcineurin phosphatase activity. Induces apoptosis.
Product Specific Literature References
X-ray crystal structure of rocaglamide, a novel antileukemic 1H-cyclopenta-(b)-benzofuran from Aglaia elliptofolia: M.L. King, et al.; J. C. S. Chem. Commun. 20, 1150 (1982)
Cyclopenta[b]benzofurans from Aglaia species with pronounced antifungal activity against rice blast fungus (Pyricularia grisea): D. Engelmeier, et al.; J. Agric. Food Chem. 48, 1400 (2000)
Insecticidal rocaglamide derivatives from Aglaia spectabilis (Meliaceae): C. Schneider, et al.; Phytochemistry 54, 731 (2000)
New insecticidal rocaglamide derivatives and related compounds from Aglaia oligophylla: M. Dreyer, et al.; J. Nat. Prod. 64, 415 (2001)
Rocaglamides, glycosides, and putrescine bisamides from Aglaia dasyclada: Chaidir, et al.; J. Nat. Prod. 64, 1216 (2001) Abstract
Rocaglamide derivatives are potent inhibitors of NF-kappa B activation in T-cells: B. Baumann, et al.; J. Biol. Chem. 277, 44791 (2002) Abstract; Full Text
Rocaglamide derivatives are immunosuppressive phytochemicals that target NF-AT activity in T cells: P. Proksch, et al.; J. Immunol. 174, 7075 (2005) Abstract; Full Text
Potential of cyclopenta[b]benzofurans from Aglaia species in cancer chemotherapy: S. Kim, et al.; Anticancer Agents Med. Chem. 6, 319 (2006)
Potent cytotoxic rocaglamide derivatives from the fruits of Amoora cucullata: P. Chumkaew, et al.; Chem. Pharm. Bull. 54, 1344 (2006)
The traditional Chinese herbal compound rocaglamide preferentially induces apoptosis in leukemia cells by modulation of mitogen-activated protein kinase activities: J.Y. Zhu, et al.; Int. J. Cancer 121, 1839 (2007) Abstract
 
 
ALX-350-140 Revised 22-Aug-07
Rocaglamide AL 
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SYNONYMS 3’-4’-Methylenedioxyrocaglamide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - NF-kB Pathway Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-140-C050   50 µg 160.00 USD Add To Cart
Product Specification
FORMULA: C26H24O7
MW: 448.5
CAS NUMBER: 201212-33-1
SOURCE/HOST: Isolated from Aglaia sp.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white sticky solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by MS, 1H-NMR.

Product Description
Derivative of rocaglamide (Prod. No. ALX-350-121) with similar pharmacological properties.
Product Specific Literature References
X-ray crystal structure of rocaglamide, a novel antileukemic 1H-cyclopenta-(b)-benzofuran from Aglaia elliptofolia: M.L. King, et al.; J. C. S. Chem. Commun. 20, 1150 (1982)
Cyclopenta[b]benzofurans from Aglaia species with pronounced antifungal activity against rice blast fungus (Pyricularia grisea): D. Engelmeier, et al.; J. Agric. Food Chem. 48, 1400 (2000)
Insecticidal rocaglamide derivatives from Aglaia spectabilis (Meliaceae): C. Schneider, et al.; Phytochemistry 54, 731 (2000) Abstract
New insecticidal rocaglamide derivatives and related compounds from Aglaia oligophylla: M. Dreyer, et al.; J. Nat. Prod. 64, 415 (2001)
Rocaglamides, glycosides, and putrescine bisamides from Aglaia dasyclada: Chaidir, et al.; J. Nat. Prod. 64, 1216 (2001) Abstract
Rocaglamide derivatives are potent inhibitors of NF-kappa B activation in T-cells: B. Baumann, et al.; J. Biol. Chem. 277, 44791 (2002) Abstract; Full Text
Rocaglamide derivatives are immunosuppressive phytochemicals that target NF-AT activity in T cells: P. Proksch, et al.; J. Immunol. 174, 7075 (2005) Abstract; Full Text
Potential of cyclopenta[b]benzofurans from Aglaia species in cancer chemotherapy: S. Kim, et al.; Anticancer Agents Med. Chem. 6, 319 (2006) Abstract
Potent cytotoxic rocaglamide derivatives from the fruits of Amoora cucullata: P. Chumkaew, et al.; Chem. Pharm. Bull. 54, 1344 (2006)
 
 
ALX-350-141 Revised 22-Aug-07
Rocaglamide C
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SYNONYMS 3’-Hydroxyrocaglamide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - NF-kB Pathway Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-141-C050   50 µg 160.00 USD Add To Cart
Product Specification
FORMULA: C29H31NO8
MW: 521.6
CAS NUMBER: 189322-67-6
SOURCE/HOST: Isolated from Aglaia sp.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white sticky solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by MS, 1H-NMR.

Product Description
Derivative of rocaglamide (Prod. No. ALX-350-121) with similar pharmacological properties.
Product Specific Literature References
X-ray crystal structure of rocaglamide, a novel antileukemic 1H-cyclopenta-(b)-benzofuran from Aglaia elliptofolia: M.L. King, et al.; J. C. S. Chem. Commun. 20, 1150 (1982)
Cyclopenta[b]benzofurans from Aglaia species with pronounced antifungal activity against rice blast fungus (Pyricularia grisea): D. Engelmeier, et al.; J. Agric. Food Chem. 48, 1400 (2000)
Insecticidal rocaglamide derivatives from Aglaia spectabilis (Meliaceae): C. Schneider, et al.; Phytochemistry 54, 731 (2000)
New insecticidal rocaglamide derivatives and related compounds from Aglaia oligophylla: M. Dreyer, et al.; J. Nat. Prod. 64, 415 (2001)
Rocaglamides, glycosides, and putrescine bisamides from Aglaia dasyclada: Chaidir, et al.; J. Nat. Prod. 64, 1216 (2001) Abstract
Rocaglamide derivatives are potent inhibitors of NF-kappa B activation in T-cells: B. Baumann, et al.; J. Biol. Chem. 277, 44791 (2002) Abstract; Full Text
Rocaglamide derivatives are immunosuppressive phytochemicals that target NF-AT activity in T cells: P. Proksch, et al.; J. Immunol. 174, 7075 (2005) Abstract; Full Text
Potential of cyclopenta[b]benzofurans from Aglaia species in cancer chemotherapy: S. Kim, et al.; Anticancer Agents Med. Chem. 6, 319 (2006) Abstract
Potent cytotoxic rocaglamide derivatives from the fruits of Amoora cucullata: P. Chumkaew, et al.; Chem. Pharm. Bull. 54, 1344 (2006)
 
 
ALX-350-142 Revised 22-Aug-07
Rocaglamide I
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SYNONYMS 1-Acetyl-3’-hydroxyrocaglamide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - NF-kB Pathway Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-142-C050   50 µg 160.00 USD Add To Cart
Product Specification
FORMULA: C31H33NO9
MW: 563.6
CAS NUMBER: 189322-68-7
SOURCE/HOST: Isolated from Aglaia sp.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white sticky solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by MS, 1H-NMR.

Product Description
Derivative of rocaglamide (Prod. No. ALX-350-121) with similar pharmacological properties.
Product Specific Literature References
X-ray crystal structure of rocaglamide, a novel antileukemic 1H-cyclopenta-(b)-benzofuran from Aglaia elliptofolia: M.L. King, et al.; J. C. S. Chem. Commun. 20, 1150 (1982)
Cyclopenta[b]benzofurans from Aglaia species with pronounced antifungal activity against rice blast fungus (Pyricularia grisea): D. Engelmeier, et al.; J. Agric. Food Chem. 48, 1400 (2000)
Insecticidal rocaglamide derivatives from Aglaia spectabilis (Meliaceae): C. Schneider, et al.; Phytochemistry 54, 731 (2000)
New insecticidal rocaglamide derivatives and related compounds from Aglaia oligophylla: M. Dreyer, et al.; J. Nat. Prod. 64, 415 (2001)
Rocaglamides, glycosides, and putrescine bisamides from Aglaia dasyclada: Chaidir, et al.; J. Nat. Prod. 64, 1216 (2001) Abstract
Rocaglamide derivatives are potent inhibitors of NF-kappa B activation in T-cells: B. Baumann, et al.; J. Biol. Chem. 277, 44791 (2002) Abstract; Full Text
Rocaglamide derivatives are immunosuppressive phytochemicals that target NF-AT activity in T cells: P. Proksch, et al.; J. Immunol. 174, 7075 (2005) Abstract; Full Text
Potential of cyclopenta[b]benzofurans from Aglaia species in cancer chemotherapy: S. Kim, et al.; Anticancer Agents Med. Chem. 6, 319 (2006) Abstract
Potent cytotoxic rocaglamide derivatives from the fruits of Amoora cucullata: P. Chumkaew, et al.; Chem. Pharm. Bull. 54, 1344 (2006)
 
 
ALX-350-143 Revised 22-Aug-07
Rocaglamide J
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SYNONYMS Aglafolin
2-Methylrocaglate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - NF-kB Pathway Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-143-C050   50 µg 160.00 USD Add To Cart
Product Specification
FORMULA: C28H28O8
MW: 492.5
CAS NUMBER: 147059-47-0
SOURCE/HOST: Isolated from Aglaia sp.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white sticky solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by MS, 1H-NMR.

Product Description
Derivative of rocaglamide (Prod. No. ALX-350-121) with similar pharmacological properties.
Product Specific Literature References
X-ray crystal structure of rocaglamide, a novel antileukemic 1H-cyclopenta-(b)-benzofuran from Aglaia elliptofolia: M.L. King, et al.; J. C. S. Chem. Commun. 20, 1150 (1982)
Cyclopenta[b]benzofurans from Aglaia species with pronounced antifungal activity against rice blast fungus (Pyricularia grisea): D. Engelmeier, et al.; J. Agric. Food Chem. 48, 1400 (2000) Abstract
Insecticidal rocaglamide derivatives from Aglaia spectabilis (Meliaceae): C. Schneider, et al.; Phytochemistry 54, 731 (2000) Abstract
New insecticidal rocaglamide derivatives and related compounds from Aglaia oligophylla: M. Dreyer, et al.; J. Nat. Prod. 64, 415 (2001) Abstract
Rocaglamides, glycosides, and putrescine bisamides from Aglaia dasyclada: Chaidir, et al.; J. Nat. Prod. 64, 1216 (2001) Abstract
Rocaglamide derivatives are potent inhibitors of NF-kappa B activation in T-cells: B. Baumann, et al.; J. Biol. Chem. 277, 44791 (2002) Abstract; Full Text
Rocaglamide derivatives are immunosuppressive phytochemicals that target NF-AT activity in T cells: P. Proksch, et al.; J. Immunol. 174, 7075 (2005) Abstract; Full Text
Potential of cyclopenta[b]benzofurans from Aglaia species in cancer chemotherapy: S. Kim, et al.; Anticancer Agents Med. Chem. 6, 319 (2006) Abstract
Potent cytotoxic rocaglamide derivatives from the fruits of Amoora cucullata: P. Chumkaew, et al.; Chem. Pharm. Bull. 54, 1344 (2006) Abstract; Full Text